Updated on 2024/07/12

写真a

 
Kinoshita Takayoshi
 
Organization
Graduate School of Science Department of Biological Chemistry Professor
School of Science Department of Biological Chemistry
Title
Professor
Affiliation
Institute of Science
Contact information
メールアドレス
Affiliation campus
Nakamozu Campus

Position

  • Graduate School of Science Department of Biological Chemistry 

    Professor  2022.04 - Now

  • School of Science Department of Biological Chemistry 

    Professor  2022.04 - Now

Degree

  • 博士(工学) ( Others )

Research Areas

  • Life Science / Pharmaceutical chemistry and drug development sciences  / Medicinal Chemistry

  • Life Science / Structural biochemistry  / Strucutral Biology

  • Life Science / Pharmaceutical chemistry and drug development sciences

  • Life Science / Structural biochemistry

  • Nanotechnology/Materials / Chemical biology

Research Interests

  • protein kinases

  • Structural Biology

  • シグナル伝達

  • X線結晶構造解析

  • Structure-based drug discovery

Research subject summary

  • キナーゼの活性制御における分子メカニズム解明と創薬

Professional Memberships

  • 日本ペプチド学会

    2016.04 - Now   Domestic

  • CBI学会

    2013.04 - Now   Domestic

  • American Chemical Society

    2005.04 - Now   Overseas

  • 日本蛋白質科学会

    2005.04 - Now   Domestic

  • 日本生化学会

    2005.04 - Now   Domestic

  • 日本薬学会

    1994.04 - Now   Domestic

  • 日本結晶学会

    1994.04 - Now   Domestic

▼display all

Committee Memberships (off-campus)

  • 2024年度大会プログラム委員   CBI学会  

    2024.01 - Now 

  • 広報委員   日本結晶学会  

    2020.04 - 2022.03 

  • 関西支部運営委員   CBI学会  

    2015.04 - Now 

Awards

  • 第10回日本蛋白質科学会年会ポスター賞

    2010.06   日本蛋白質科学会  

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    Country:Japan

  • 構造活性相関シンポジウムポスター賞

    2008   日本薬学会構造活性相関部会  

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    Country:Japan

  • Breakthrough award, division of medicinal chemistry, PSJ in 2005

    2005.11  

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    Country:Japan

Papers

  • Distinct binding modes of a benzothiazole derivative confer structural bases for increasing ERK2 or p38α MAPK selectivity Reviewed

    S. Hasegawa, M. Yoshida, H. Nagao, H. Sugiyama, M. Sawa, T. Kinoshita

    Biochem. Biophys. Res. Commun.   704   149707 - 149707   2024.02

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    Authorship:Last author, Corresponding author   Publishing type:Research paper (scientific journal)   International / domestic magazine:International journal  

  • Low entropic cost of binding confers high selectivity on an allosteric ERK2 inhibitor Reviewed

    H. Sugiyama, M. Yoshida, H. Nagao, M. Sawa, T. Kinoshita,

    Bioorg. Med. Chem. Lett.   93   129431 - 129431   2023.08

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    Authorship:Last author, Corresponding author   Publishing type:Research paper (scientific journal)   International / domestic magazine:International journal  

  • Design, synthesis and structure-activity relationship studies of protein kinase CK2 inhibitors containing a purine scaffold Reviewed

    2. K. Nishiwaki, S. Nakamura, K. Yoshioka, E. Nakagawa, S. Nakatani, M. Tsuyuguchi, T. Kinoshita, I. Nakanishi

    Chem. Pharm. Bull.   71   558 - 565   2023.07

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    Publishing type:Research paper (scientific journal)   International / domestic magazine:International journal  

  • Bivalent binding mode of an amino-pyrazole inhibitor indicates the potentials for CK2α1-selective inhibitors.

    Asaka Ikeda, Masato Tsuyuguchi, Daisuke Kitagawa, Masaaki Sawa, Shinya Nakamura, Isao Nakanishi, Takayoshi Kinoshita

    Biochemical and biophysical research communications   630   30 - 35   2022.11( ISSN:0006291X

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    Publishing type:Research paper (scientific journal)   International / domestic magazine:International journal  

    Casein kinase 2 (CK2) is a vital protein kinase that consists of two catalytic subunits (CK2α1 and/or CK2α2) and two regulatory subunits (CK2β). CK2α1 is a drug target for nephritis and cancers, while CK2α2 is a serious off-target because its inhibition causes testicular toxicity. High similarity between the isozymes CK2α1 and CK2α2 make it difficult to design CK2α1-specific inhibitors. Herein, the crystal structures of CK2α1 and CK2α2 complexed with a 3-amino-pyrazole inhibitor revealed the remarkable differences in the protein-inhibitor interaction modes. This inhibitor bound to the ATP binding sites of both isozymes in apparently distinct orientations. In addition, another molecule of this inhibitor bound to CK2α1, but not to CK2α2, at the CK2β protein-protein interface. Binding energy calculations and biochemical experiments suggested that this inhibitor possesses the conventional ATP-competitive characteristics with moderate allosteric function in a molecular glue mechanism. These results will assist the potential design of potent and selective CK2α1 inhibitors.

    DOI: 10.1016/j.bbrc.2022.09.040

    PubMed

  • Identification of a novel target site for ATP-independent ERK2 inhibitors Reviewed

    M. Yoshida, H. Nagao, H. Sugiyama, M. Sawa, T. Kinoshita

    Biochem. Biophys. Res. Commun.   593   73 - 78   2022.04

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    Authorship:Last author, Corresponding author   Publishing type:Research paper (scientific journal)   International / domestic magazine:International journal  

  • Identification of an allosteric and Smad3-selective inhibitor of p38aMAPK using a substrate-based approach Reviewed

    H. Nagao, D. Kitagawa, F. Nakajima, M. Sawa, T. Kinoshita

    Bioorg. Med. Chem. Lett. 雑誌   31   2021.04

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    Kind of work:Joint Work  

  • Structural basis for producing selective MAP2K7 inhibitors Reviewed

    Y. Murakawa, S. Valter, H. Barr, N. London, T. Kinoshita

    Bioorg. Med. Chem. Lett. 雑誌   30   2020.11

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    Kind of work:Joint Work  

  • Structural insights for producing CK2a1-specific inhibitors Reviewed

    M. Tsuyuguchi, T. Nakaniwa, A. Hirasawa, I. Nakanishi, T. Kinoshita

    Bioorg. Med. Chem. Lett. 雑誌   30   2020.02

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    Kind of work:Joint Work  

  • Ensemble structural analyses depict the regulatory mechanism of non-phosphorylated human MAP2K4 Reviewed

    T. Matsumoto, A. Yamano, Y. Murakawa, H. Fukada, M. Sawa, T. Kinoshita

    Biochem. Biophys. Res. Commun. 雑誌   521   106 - 112   2020.01

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    Kind of work:Joint Work  

  • An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue Reviewed

    N. Furuya, T. Momose, K. Katsuno, N. Fushimi, H. Muranaka, C. Handa, M. Sawa, T. Ozawa, T. Kinoshita

    Bioorg. Med. Chem. Lett. 雑誌   30   2020.01

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    Kind of work:Joint Work  

  • Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth

    Tsuyoshi Oshima, Yoshimi Niwa, Keiko Kuwata, Ashutosh Srivastava, Tomoko Hyoda, Yoshiki Tsuchiya, Megumi Kumagai, Masato Tsuyuguchi, Teruya Tamaru, Akiko Sugiyama, Natsuko Ono, Norjin Zolboot, Yoshiki Aikawa, Shunsuke Oishi, Atsushi Nonami, Fumio Arai, Shinya Hagihara, Junichiro Yamaguchi, Florence Tama, Yuya Kunisaki, Kazuhiro Yagita, Masaaki Ikeda, Takayoshi Kinoshita, Steve A. Kay, Kenichiro Itami, Tsuyoshi Hirota

    Science Advances   5 ( 1 )   2019.01( eISSN:2375-2548

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    Publishing type:Research paper (scientific journal)  

    Copyright © 2019 The Authors, some rights reserved. Compounds targeting the circadian clock have been identified as potential treatments for clock-related diseases, including cancer. Our cell-based phenotypic screen revealed uncharacterized clock-modulating compounds. Through affinity-based target deconvolution, we identified GO289, which strongly lengthened circadian period, as a potent and selective inhibitor of CK2. Phosphoproteomics identified multiple phosphorylation sites inhibited by GO289 on clock proteins, including PER2 S693. Furthermore, GO289 exhibited cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function. The x-ray crystal structure of the CK2-GO289 complex revealed critical interactions between GO289 and CK2-specific residues and no direct interaction of GO289 with the hinge region that is highly conserved among kinases. The discovery of GO289 provides a direct link between the circadian clock and cancer regulation and reveals unique design principles underlying kinase selectivity.

    DOI: 10.1126/sciadv.aau9060

    PubMed

  • Covalent docking identifies a potent and selective MKK7 inhibitor Reviewed

    A. Shraga, E. Olhavang, N. Davidzohn, P. Khoshkenar, N. Germain, K. Shurrush, S. Carvalho, L. Avram, S. Albeck, T. Unger, B. Lefker, C. Subramanyam, R.H. Hudkins, A. Mitchell, Z. Shulman, T. Kinoshita, N. London

    Cell Chem. Biol. 雑誌   26   98 - 108   2019.01

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    Kind of work:Joint Work  

  • A microgravity environment improves structural resolution and endows cues for specific inhibition of mitogen-activated protein kinase kinase 7 Reviewed

    T. Kinoshita, T. Hashimoto, Y. Murakawa, Y. Sogabe, T. Matsumoto, M. Sawa

    Int. J. Microgravity Sci. Appl. 雑誌   36   2019.01

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    Kind of work:Joint Work  

  • A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1

    Masato Tsuyuguchi, Tetsuko Nakaniwa, Masaaki Sawa, Isao Nakanishi, Takayoshi Kinoshita

    Acta Crystallographica Section F: Structural Biology Communications   75   515 - 519   2019( eISSN:2053-230X

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    Publishing type:Research paper (scientific journal)  

    © 2019 International Union of Crystallography. Protein kinase CK2a1 is a serine/threonine kinase that plays a crucial role in the growth, proliferation and survival of cells and is a well known target for tumour and glomerulonephritis therapies. Here, the crystal structure of the kinase domain of CK2a1 complexed with 5-iodotubercidin (5IOD), an ATP-mimetic inhibitor, was determined at 1.78 Å resolution. The structure shows distinct structural features and, in combination with a comparison of the crystal structures of five off-target kinases complexed with 5IOD, provides valuable information for the development of highly selective inhibitors.

    DOI: 10.1107/S2053230X19008951

    PubMed

  • Hydration structures of the human protein kinase CK2a clarified by joint neutron and X-ray crystallography Reviewed

    C. Shibasaki, S. Arai, R. Shimizu, M. Saeki, T. Kinoshita, A. Ostermann, T.E. Schrader, Y. Kurosaki, T. Sunami, R. Kuroki, M. Adachi

    J. Mol. Biol. 雑誌   430   5094 - 5104   2018.07

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    Kind of work:Joint Work  

  • Crystal structures of human CK2a2 in new crystal forms arising from a subtle difference in salt concentration Reviewed

    M. Tsuyuguchi, T. Nakaniwa, T. Kinoshita

    Acta Cryst. 雑誌   F74   288 - 293   2018.06

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    Kind of work:Joint Work  

  • Foretinib overcomes entrectinib resistance associated with the NTRK1 G667C mutation in NTRK1 fusion-positive tumor cells in a brain metastasis model Reviewed

    A. Nishiyama, T. Yamada, K. Kita, R. Wang, S. Arai, K. Fukuda, A. Tanimoto, S. Takeuchi, S. Tange, A. Tajima, N. Furuya, T. Kinoshita, S. Yano

    Clinical Cancer Res. 雑誌   24   2357 - 2369   2018.05

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    Kind of work:Joint Work  

  • High-resolution structure discloses the potential for allosteric regulation of mitogen-activated protein kinase kinase 7 Reviewed

    T. Kinoshita, T. Hashimoto, Y. Sogabe, H. Fukada, T. Matsumoto, M. Sawa

    Biochem. Biophys. Res. Commun. 雑誌   493   313 - 317   2017.06

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    Kind of work:Joint Work  

  • The juxtamembrane region of TrkA kinase is critical for inhibitor selectivity Reviewed

    N. Furuya, T. Momose, K. Katsuno, N. Fushimi, H. Muranaka, C. Handa, T. Ozawa, T. Kinoshit

    Bioorg. Med. Chem. Lett. 雑誌   27   1233 - 1236   2017.01

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    Kind of work:Joint Work  

  • A crucial role of Cys218 in configuring an unprecedented auto-inhibition form of MAP2K7 Reviewed

    Y. Sogabe, T. Hashimoto, T. Matsumoto, Y. Kirii, M. Sawa, T. Kinoshita

    Biochem. Biophys. Res. Commun. 雑誌   473   476 - 481   2016.10

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  • Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inihibitors Reviewed

    H. Ohno, D. Minamiguchi, S. Nakamura, K. Shu, S. Okazaki, M. Honda, R. Misu, H. Moriwaki, S. Nakanishi, S. Oishi, T. Kinoshita, I. Nakanishi, N. Fujii

    Bioorg. Med. Chem. 雑誌   24   1136 - 1141   2016.03

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    Kind of work:Joint Work  

  • Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay Reviewed

    T. Kinoshita, H. Sugiyama, Y. Mori, N. Takahashi, A. Tomonaga

    Bioorg. Med. Chem. Lett. 雑誌   26   955 - 958   2016.02

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    Kind of work:Joint Work  

  • Bioconversion of FR901459, a novel derivative of cyclosporine A, by Lenzea sp. 7887 Reviewed

    S. Sasamura, M. Kobayashi, H. Muramatsu, S. Yoshimura, T. Kinoshita, H. Ohki, K. Okada, Y. Deai, Y. Yamagishi, M. Hashimoto

    J. Antibiot. 雑誌   68   511 - 520   2015.07

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    Kind of work:Joint Work  

  • Identification of protein kinase CK2 inhibitors using solvent dipole ordering virtual screening Reviewed

    I. Nakanishi, K. Murata, N. Nagata, M. Kurono, T. Kinoshita, M. Yasue, T. Miyazaki, Y. Takei, S. Nakamura, A. Sakurai, N. Iwamoto, N. Nishiwaki, T. Nakaniwa, Y. Sekiguchi, A. Hirasawa, G. Tsujimoto, K. Kitaura

    Eur. J. Med. Chem. 雑誌   96   396 - 404   2015.04

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  • 5Z-7-oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner Reviewed

    Y. Sogabe, T. Matsumoto, T. Hashimoto, Y. Kirii, M. Sawa, T. Kinoshita

    Bioorg. Med. Chem. Lett.   25   593 - 596   2015.01

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    Kind of work:Joint Work  

  • Hepatocyte growth factor Reviewed

    K. Sakai, T. Kinoshita, K. Matsumoto

    References Module in Biological Sciences   2014.12

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    Kind of work:Joint Work  

  • Crystal structure of human CK2a at 1,06A resolution Reviewed

    T. Kinoshita, T. Nakaniwa, Y. Sekiguchi, Y. Sogabe, A. Sakurai, S. Nakamura, I. Nakanishi

    J. Synchrotron Rad.   20   974 - 979   2013.12

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    Kind of work:Joint Work  

  • ヒトMAPキナーゼJNK1の立体構造・機能・安定性に対する遊離システイン残基の置換効果 Reviewed

    仲庭哲津子、深田はるみ、黒木良太、木下誉富

    日本結晶学会誌 日本結晶学会   55   197 - 202   2013.06

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  • Seven cysteine-deficient mutants depict interplay between thermal and chemical stabilities of individual cysteine residues in MAP kinase JNK1 Reviewed

    T. Nakaniwa, H. Fukada, T. Inoue, M. Gouda, R. Nakai, Y. Kirii, M. Adachi, T. Tamada, S. Segawa, R. Kuroki, T. Tada, T. Kinoshita

    Biochemistry   51   8410 - 8421   2012.10

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  • Crystal and solution structures disclose a putative transient state of mitogen-activated kinase kinase 4 Reviewed

    T. Matsumoto, T. Kinoshita, Y. Kirii, T. Tada, A. Yamano

    Biochem. Biophys. Res. Commun.   425   195 - 200   2012.08

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  • The in silico screening and X-ray structure analysis and the inhibitor complex of plasmodium falciparum orotidine-5'-monophosphate decarboxylase Reviewed

    Y. Takashima, E. Mizohata, S.R. Krunkrai, Y. Fukunishi, T. Kinoshita, T. Sakata, H. Matsumra, J. Krungkrai, T. Horii, T. Inoue

    J. Biochem.   152   133 - 138   2012.08

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  • Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state Reviewed

    T. Matsumoto, T. Kinoshita, H. Furukawa, R. Nakai, Y. Kirii, K. Yokota, T. Tada

    J. Biochem.   151   541 - 549   2012.05

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  • Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scafolds Reviewed

    Z. Hou, I. Nakanishi, T. Kinoshita, Y. Takei, M. Yasue, R. Misu, Y. Suzuki, S. Nakamura, T. Kure, H. Ohno, K. Murata, K. Kitaura, A. Hirasawa, G. Tsujimoto, S. Oishi, N. Fujii

    J. Med. Chem.   55   2899 - 2903   2012.03

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  • Knowledge-based identification of the ERK2/STAT3 signal pathway as a therapeutic target for type 2 diabates and drug discovery Reviewed

    T. Kinoshita, K. Doi, H. Sugiyama, S. Kinoshita, M. Wada, S. Naruto, T. Tomonaga

    Chem. Biol. Drug Des.   78   471 - 476   2011.09

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  • A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase Reviewed

    T. Kinoshita, Y. Sekiguchi, H. Fukada, T. Nakaniwa, T. Tada, S. Nakamura, K. Kitaura, H. Ohno, Y. Suzuki, A. Hirasawa, I. Nakanishi, G. Tsujimoto

    Mol. Cell. Biochem.   356   97 - 105   2011.09

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    Kind of work:Joint Work  

  • HGF-antagonists: structure, activities, and anti-cancer approach Reviewed

    K. Sakai, T. Nakamura, T. Kinoshita, T. Nakamura, K. Matsumoto

    Current Signal Transduction Therapy   6   191 - 199   2011.05

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    Kind of work:Joint Work  

  • High resolution structure of exo-arabinanase from Penicillium chrysogenum Reviewed

    Y. Sogabe, T. Kitatani, A. Yamaguchi, T. Kinoshita, H. Adachi, K. Takano, T. Inoue, Y. Mori, H. Matsumura, T. Sakamoto, T. Tada

    Acta Cryst.   D67   415 - 422   2011.04

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    Kind of work:Joint Work  

  • Crystal structures of MKK4 kinase domain reveal that substrate peptide binds to an allosteric site and induces an auto-inhibition state Reviewed

    T. Matsumoto, T. Kinoshita, Y. Kirii, K. Yokota, K. Hamada, T. Tada

    Biochem. Biophys. Res. Commun.   400   369 - 373   2010.08

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    Kind of work:Joint Work  

  • 中性子構造解析および超高分解能X線構造解析によるエラスターゼの機能解明 Reviewed

    玉田太郎、黒木良太、木下誉富、多田俊治

    日本結晶学会誌 日本結晶学会   52 ( 2 )   133 - 138   2010.04

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  • A silent mutation allows efficient production of active human Frk tyrosine kinase in Escheria coli Reviewed

    X. Yang, T. Kinoshita, M. Gouda, K. Yokota, T. Tada

    Biosci. Biotechnol. Biochem.   74   125 - 128   2010.02

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    Kind of work:Joint Work  

  • 創薬バリューチェインのインシリコ技術を活用した阻害剤開発の試み Reviewed

    井上豪、松村浩由、安達宏昭、森勇介、高野和文、村上聡、福西快文、中村春木、木下誉富、仲西功、奥野恭史、南方聖司、三上義明、佐久間俊広、北島正人、福岡良忠、高田俊和、坂田恒昭

    日本結晶学会誌 日本結晶学会   52 ( 1 )   89 - 94   2010.02

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  • Structure basis for the inhibitor recognition of human Lyn kinase domain Reviewed

    N. Miyano, T.Kinoshita, R. Nakai, Y. Kirii, K. Yokota, T. Tada

    Bioorg. Med. Chem. Lett.   19   6557 - 6560   2009.11

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  • Combined high-resolution neutron and X-ray analysis of inhibited elastase confirms the active-site oxyanion hole but rules against a low-barrier hydrogen bond Reviewed

    T. Tamada, T. Kinoshita, K. Kurihara, M. Adachi, T. Ohhara, K. Imai, R. Kuroki, T. Tada

    J. Am. Chem. Soc.   131   11033 - 11040   2009.08

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  • Structural insight into human CK2a in complex with the potent inhibitor ellagic acid Reviewed

    Y. Sekiguchi, T. Nakaniwa, T. Kinoshita, I. Nakanishi, K. Kitaura, A. Hirasawa, G. Tsujimoto, T. Tada

    Bioorg. Med. Chem. Lett.   19   2920 - 2923   2009.05

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  • Structure of human protein kinase CK2a2 with a potent indazole-derivative inhibitor Reviewed

    T. Nakaniwa, T. Kinoshita, Y. Sekiguchi, T. Tada, I. Nakanishi, K. Kitaura, Y. Suzuki, H. Ohno, A. Hirasawa, G. Tsujimoto

    Acta Cryst.   F65   75 - 79   2009.02

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  • Crystal structure of human mono-phosphorylated ERK1 at Tyr204 Reviewed

    T. Kinoshita, I. Yoshida, S. Nakae, K. Okita, M. Gouda, M. Matsubara, K. Yokota, H. Ishiguro, T. Tada

    Biochem. Biophys. Res. Commun.   377   1123 - 1127   2008.12

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    Kind of work:Joint Work  

  • Conformation change of adenosine deaminase during ligand-exchange in a crystal Reviewed

    T. Kinoshita, T. Tada, I. Nakanishi

    Biochem. Biophys. Res. Commun.   373   53 - 57   2008.07

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  • Protein purification and preliminary crystallographic analysis of human Lyn tyrosine kinase Reviewed

    T. Kinoshita, N. Miyano, R. Nakai, K. Yokota, H. Ishiguro, T. Tada

    Protein Expr. Purif.   58   318 - 324   2008.03

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  • Crystallization of porcine pancreatic elastase and preliminary neutron diffraction experiment Reviewed

    T. Kinoshita, T. Tamada, K. Imai, K. Kurihara, T. Ohhara, T. Tada, R. Kuroki

    Acta Cryst.   F63   315 - 317   2007.04

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  • Role of a cystein residue in the active site of ERK and the MAPKK family Reviewed

    M. Ohori, T. Kinoshita, S. Yoshimura, M. Warizaya, H. Nakajima, H. Miyake

    Biochem. Biophys. Res. Commun.   353   633 - 637   2007.02

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  • Structure of human Fyn kinase domain complexed with staurosporine Reviewed

    T. Kinoshita, M. Matsubara, H. Ishiguro, K. Okita, T. Tada

    Biochem. Biophys. Res. Commun.   346   840 - 844   2006.08

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  • Structure of apo-glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7992 Reviewed

    T. Kitatani, Y. Nakamura, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, T. Tada

    Acta Cryst.   F62   727 - 730   2006.08

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  • Tris(hydroxymethyl)aminomethane induces conformational change and crystal-packing contraction of porcine pancreatic elastase Reviewed

    T. Kinoshita, A. Yamaguchi, T. Tada

    Acta Cryst.   F62   623 - 626   2006.07

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  • Anti-inflammatory activity of non-nucleoside adenosine deaminase inhibitor FR234938 Reviewed

    M. Kuno, N. Seki, S. Tsujimoto, I. Nakanishi, T. Kinoshita, K. Nakamura, T. Terasaka, N. Nishio, A. Sato, T. Fujii

    Eur. J. Pharmcol.   534   241 - 249   2006.04

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  • Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling Reviewed

    J. Ishida, H. Yamamoto, Y. Kido, K. Kamijo, K. Murano, H. Miyake, M. Okubo, T. Kinoshita, M. Warizaya, A. Iwashita, K. Mihara, N. Matsuoka, K. Hattori

    Bioorg. Med. Chem.   14   1378 - 1390   2006.03

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  • Structure of NADP-dependent glyceraldehyde-3-phosphate dehydrogenase from Synechococcus PCC7942 complexed with NADP Reviewed

    T. Kitatani, Y. Nakamura, K. Wada, T. Kinoshita, S. Shigeoka, T. Tada

    Acta Cryst.   F62   315 - 319   2006.03

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  • Crystal structure of human ERK2 complexed with a pyrazolo[3,4c]pyridazine derivative Reviewed

    T. Kinoshita, M. Warizaya, M. Ohori, K. Sato, M. Neya, T. Fujii

    Bioorg.Med. Chem. Lett.   16   55 - 58   2006.01

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  • Solution-Stirring Method Improves Crystal Quality of Human Triosephosphate Isomerase Reviewed

    H. Adachi, A. Niino, T. Kinoshita, M. Warizaya, R. Maruki, K. Takano, H. Matsumura, T. Inoue, S. Murakami, Y. Mori, T. Sasaki

    J. Biosci. Bioeng.   101   83 - 86   2006.01

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    Kind of work:Joint Work  

  • Protein Crystallization by combining laser irradiation and solution-stirring techniques Reviewed

    H. Adachi, A. Niino, S. Murakami, K. Takano, H. Matsumura, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori and T. Sasaki

    Jpn. J. Appl. Phys.   44   1365 - 1366   2005.12

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  • Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitors Reviewed

    A. Iwashita, K. Hattori, H. Yamamoto, J. Ishida, Y. Kido, K. Kamijo, K. Murano, H. Miyake, T. Kinoshita, M. Warizaya, M. Ohkubo, N. Matsuoka, S. Mutoh

    FEBS Letters   579   1389 - 1393   2005.11

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  • Structure of the complex of porcine pancreatic elastase with a trimacrocyclic peptide inhibitor FR901451 Reviewed

    T. Kinoshita, T. Kitatani, M. Warizaya, T. Tada

    Acta Cryst.   F61   808 - 811   2005.08

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  • Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism Reviewed

    T. Terasaka, K. Tsuji, T. Kato, I. Nakanishi, T. Kinoshita, Y. Kato, M. Kuno, T. Inoue, K. Tanaka and K. Nakamura

    J. Med. Chem.   48   4750 - 4753   2005.08

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    Kind of work:Joint Work  

  • Structural basis of compound recognition by adenosine deaminase Reviewed

    T. Kinoshita, I. Nakanishi, T. Terasaka, M. Kuno, N. Seki, M. Warizaya, H. Matsumura, T. Inoue, K. Takano, H. Adachi, Y. Mori, T. Fujii

    Biochemistry   44   10562 - 10569   2005.08

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  • FR177391, a new anti-hyperlipidemic agent from Serratia Reviewed

    B. Sato, H. Nakajima, T. Fujita, S. Takase, S. Yoshimura, T. Kinoshita, H. Terano

    J. Antibiot.   58   634 - 639   2005.06

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  • Structure of a high-resolution crystal form of human triosephosphate isomerase: improvement of crystals using the gel-tube method Reviewed

    T. Kinoshita, R. Maruki, M. Warizaya, H. Nakajima and S. Nishimura

    Acta Cryst.   F61   346 - 349   2005.06

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  • Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex Reviewed

    M. Ohori, T. Kinoshita, M. Okubo, K. Sato, A. Yamazaki, H. Arakawa, S. Nishimura, N. Inamura, H. Nakajima, M. Neya, T. Fujii

    Biochem. Biophys. Res. Commun.   336   357 - 363   2005.06

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  • FR207944, an Antifungal Antibiotic from Chaetomium sp. No.217. II. Isolation and Structure Elucidation Reviewed

    M. Kobayashi, S. Yoshimura, T. Kinoshita, M. Hashimoto, S. Hashimoto, S. Takase, A. Fujie, M. Hino, Y. Hori

    Biosci. Biotechnol. Biochem.   69   1029 - 1032   2005.06

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  • Solution stirring initiates nucleation and improves the quality of adenosine deaminase crystals Reviewed

    H. Adachi, K. Takano, A. Niino, H. Matsumura, T. Kinoshita, M. Warizaya, Y. Mori, T. Sasaki

    Acta Cryst.   D61   759 - 762   2005.05

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  • The novel gluconeogenesis inhibitor FR225654 that originates from Phoma sp. No. 00144 II. Structure determination Reviewed

    Y. Ohtsu, S. Yoshimura, T. Kinoshita, S. Takase, H. Nakajima

    J. Antiniot.   58   479 - 482   2005.04

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  • ヒト由来ADP-リボースポリメラーゼの立体構造解析:阻害剤結合による活性部位の構造変化 Reviewed

    木下誉富

    日本結晶学会誌 日本結晶学会   46 ( 6 )   421 - 425   2004.12

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  • Control of protein crystal nucleation and growth using stirring solution Reviewed

    A. Niino, H. Adachi, K. Takano, H. Matsumura, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori and T. Sasaki

    Jpn. J. Appl. Phys.   43   L1442 - L1444   2004.11

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  • Expression, purification, crystallization and preliminary X-ray diffraction studies of human liver regucalcin Reviewed

    M. Warizaya, T. Kinoshita, M. Yamaoka, T. Shibata, N. Saito, H. Nakajima and T. Fujii

    Acta Cryst.   D60   2019 - 2021   2004.10

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  • SmI2-mediated reduction of ?,?-difluoro-?,?-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipetide isosteres Reviewed

    A. Otaka, J. Watanabe, A. Yukimasa, Y. Sasaki, H. Watanabe, T. Kinoshita, S. Oishi, H. Tamamura, N. Fujii

    J. Org. Chem.   69   1634 - 1645   2004.08

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  • Rational approaches to discovery of orally active and brain penetrable PARP inhibitors Reviewed

    K. Hattori, Y. Kido, H. Yamamoto, J. Ishida, K. Kamijo, K. Murano, M. Ohkubo, T. Kinoshita, A. Iwashita, K. Mihara, S. Yamazaki, N. Matsuoka, Y. Teramura, H. Miyake

    J. Med. Chem.   47   4151 - 4154   2004.08

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  • Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors Reviewed

    T. Terasaka, T. Kinoshita, M. Kuno, N. Seki, K. Tanaka, I. Nakanishi

    J. Med. Chem.   47   3730 - 3743   2004.07

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  • Generation of protein crystals using a solution-stirring technique Reviewed

    H. Adachi, H. Matsumura, A. Niino, K. Takano, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori, T. Sasaki

    Jpn. J. Appl. Phys.   43   L762 - L764   2004.07

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  • Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors Reviewed

    T. Terasaka, H. Okumura, K. Tsuji, T. Kato, I. Nakanishi, T. Kinoshita, Y. Kato, M. Kuno, N. Seki, Y. Naoe, T. Inoue, K. Tanaka, K. Nakamura

    J. Med. Chem.   47   2728 - 2731   2004.06

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  • Improving the quality of protein crystals using stirring crystallization Reviewed

    H. Adachi, H. Matsumura, A. Niino, K. Takano, T. Kinoshita, M. Warizaya, T. Inoue, Y. Mori, T. Sasaki

    Jpn. J. Appl. Phys.   43   L522 - L525   2004.05

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  • Cloning, expression, purification, crystallization and preliminary diffraction analysis of human liver glyceraldehyde-3-phophate dehydrogenase Reviewed

    M. Warizaya, T. Kinoshita, A. Kato, H. Nakajima, T. Fujii

    Acta Cryst.   D60   567 - 568   2004.05

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  • Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase Reviewed

    T. Kinoshita, I. Nakanishi, M. Warizaya, A. Iwashita, Y. Kido, K. Hattori, T. Fujii

    FEBS Letters   556   43 - 46   2004.01

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  • Cloning, expression, purification, crystallization and preliminary diffraction analysis of the C-terminal catalytic domain of human poly(ADP-ribose) polymerase Reviewed

    T. Kinoshita, T. Tsutsumi, R. Maruki, M. Warizaya, Y. Ishii, T. Fujii

    Acta Cryst.   D60   109 - 111   2004.01

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  • A highly potent non-nucleotide adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization Reviewed

    T. Terasaka, T. Kinoshita, M. Kuno, I. Nakanishi

    J. Am. Chem. Soc.   126   34 - 35   2004.01

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  • Improving quality and harvest period of protein crystals for structure based drug design: effects of a gel and a magnetic field on bovine adenosine deaminase crystals Reviewed

    T. Kinoshita, M. Ataka, M. Warizaya, M. Neya, T. Fujii

    Acta Cryst.   D59   1333 - 1335   2003.06

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  • Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors Reviewed

    T. Terasaka, I. Nakanishi, K. Nakamura, Y. Eikyu, T. Kinoshita, N. Nishio, A. Sato, M. Kuno, N. Seki, K. Sakane

    Bioorg. Med. Chem. Lett.   13   1115 - 1118   2003.06

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  • FR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase III. Structure determination Reviewed

    H. Mori, Y. Urano, T. Kinoshita, S. Yoshimura, S. Takase, M. Hino

    J. Antibiot.   56   181 - 185   2003.02

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  • Crystal structure of bovine adenosine deaminase complexed with 6-hydroxyl-1,6-dihydropurine riboside Reviewed

    T. Kinoshita, N. Nishio, I. Nakanishi, A. Sato, T. Fujii

    Acta Cryst.   D59   299 - 303   2003.02

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  • True interaction mode of porcine pancreatic elastase with FR136706, a potent peptidyl inhibitor Reviewed

    T. Kinoshita, I. Nakanishi, A. Sato, T. Tada

    Bioorg. Med. Chem. Lett.   13   21 - 24   2003.01

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  • Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-Sn2' reactions Reviewed

    A. Otaka, F. Katagiri, T. Kinoshita, Y. Odagaki, O. Shinya, H. Tamamura, N. Hamanaka N. Fuji

    J. Org. Chem.   67   6152 - 6161   2002.10

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  • Enantiometric recognition of amino acids using a chiral spiropyran derivative Reviewed

    K. Tsubaki, K. Mukoyoshi, H. Morikawa, T. Kinoshita, K. Fuji

    Chirality   14   713 - 715   2002.06

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  • Use of meso-ternaphthalene derivatives: linear recognition of the ?,?-diamines by homoditopic receptors. Synthesis of the proton-ionizable lariat crown ether and chiral recognition of primary amines Reviewed

    K. Tsubaki, H. Tanaka, T. Furuta, K. Tanaka, T. Kinoshita, K. Fuji

    Tetrahedron   58   5611 - 5617   2002.06

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  • The structure of human recombinant aldose reductase complexed with the potent inhibitor zenarestat Reviewed

    T. Kinoshita, H. Miyake, T. Fujii, S. Takakura, T. Goto

    Acta Cryst.   D58   622 - 626   2002.04

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  • Synthesis of the proton-ionizable lariat crown ether and chiral recognition of primary amines Reviewed

    K. Tsubaki, H. Tanaka, T. Kinoshita, K. Fuji

    Tetrahedron   58   1679 - 1684   2002.02

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  • Crystallization and preliminary X-ray diffraction studies of catalase-peroxidase from Synechococcus PCC 7942 Reviewed

    K. Wada, T. Tada, Y. Nakamura, T. Kinoshita, M. Tamoi, S. Shigeoka, K.Nishimura

    Acta Cryst.   D58   157 - 159   2002.01

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  • Synthesis, structure, and ion-binding properties of new tetraoxacalix[3]arenes Reviewed

    K. Tsubaki, T. Morimoto, T. Otsubo, T. Kinoshita, K. Fuji

    J. Org. Chem.   66   4083 - 4086   2001.11

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  • Crystallization and preliminary X-ray diffraction analysis of NADP-dependent glyceraldehide-3-dehydrogenase of Synechococcus PCC 7942 Reviewed

    Y. Nakamura, T. Tada, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, K. Nishimura

    Acta Cryst.   D57   879 - 881   2001.06

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  • The first example for cycloenatiomeric hexahomooxacalix[3]arenes Reviewed

    K. Tsubaki, T. Otsubo, T. Kinoshita, M. Kawada, K. Fuji

    Chem. Pharm. Bull.   49   507 - 509   2001.04

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  • Purification, crystallization and preliminary X-ray diffraction analysis of the fructose-1,6/sedoheptulose-1,7-bisphosphatase of Synechococcus PCC 7942 Reviewed

    Y. Nakamura, T. Tada, K. Wada, T. Kinoshita, M. Tamoi, S. Shigeoka, K. Nishimura

    Acta Cryst.   D57   454 - 456   2001.03

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  • Memory of chirality in diastereoselective α-alkylation of isoleucine and allo-isoleucine derivatives Reviewed

    T. Kawabata, J. Chen, H. Suzuki, Y. Nagae, T. Kinoshita, S.Chancharunee, K. Fuji

    Org. Lett.   2   3883 - 3885   2000.10

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  • Recognition of the chain length of ?,?-diamines by a meso-ternaphthalene derivative with two crown ethers Reviewed

    K. Tsubaki, H. Tanaka, T. Furuta, T. Kinoshita, K. Fuji

    Tetrahedron Lett.   41   6089 - 6093   2000.08

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  • Stereoselective synthesis of CF2-substituted phosphothreonine mimetics and their incorporation into peptides using newly developed deprotection procedures Reviewed

    A. Otaka, E. Mitsuyama, T. Kinoshita, H. Tamamura, N. Fujii

    J. Org. Chem.   65   4888 - 4899   2000.06

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  • A new antimitotic substance, FR182877 Reviewed

    S. Yoshimura, B. Sato, T. Kinoshita, S. Takase, H. Terano

    J. Antibiot.   53   615 - 622   2000.05

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  • Crystallization and preliminary X-ray analysis of cephalosporin C acylase from Pseudomonas sp. strain N176 Reviewed

    T. Kinoshita, T. Tada, Y. Saito, Y. Ishii, A. Sato, M. Murata

    Acta Cryst.   D56   458 - 459   2000.04

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  • Structure of porcine pancreatic elastase complexed with FR901277, a novel macrocyclic inhibitor of elastases, at 1.6 ? resolution Reviewed

    I. Nakanishi, T. Kinoshita, A. Sato, T. Tada

    Biopolymers   53   434 - 445   2000.03

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  • Dual CCK-A and CCK-B receptor antagonists (II). Preparation and structure activity relationships of 5-alkyl-9-methyl-1,4-benzodiazepines and discovery of FR208419 Reviewed

    S. Tabuchi, H. Ito, H. Sogabe, M. Kuno, T. Kinoshita, I. Katumi, N. Yamamoto, H. Mitsui, Y. Satoh

    Chem. Pharm. Bull.   48   1 - 15   2000.01

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  • The supramolecular structure of 1,4-bis(9-fluorenyl)-1,4-dihydro[60]fullerene with hexahomotrioxacalix[3]arene in the solid state Reviewed

    The supramolecular structure of 1,4-bis(9-fluorenyl)-1,4-dihydro[60]fullerene with hexahomotrioxacalix[3]arene in the solid state

    Hetrocycles   51   2553 - 2556   1999.12

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  • Crystallization and preliminary analysis of bovine adenosine deaminase Reviewed

    T. Kinoshita, N. Nishio, A. Sato, M. Murata

    Acta Cryst.   D55   2031 - 2032   1999.12

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  • Visualization of molecular length of ?,?-diamines and temperature by a receptor based on phenolphthalein and crown ether Reviewed

    K. Fuji, K. Tsubaki, K. Tanaka, N. Hayashi, T. Otsubo, T. Kinoshita

    J. Am. Chem. Soc.   121   3807 - 3808   1999.10

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  • Synthesis of the water-soluble adenosine A1 receptor antagonist FR166124 through a novel sequential Horner-Emmons/isomerization reaction Reviewed

    S. Kuroda, A. Akahane, H. Itani, S. Nishimura, K. Durkin, T. Kinoshita, K. Sakane

    Tetrahedron   55   10351 - 10364   1999.08

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  • Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation Reviewed

    I. Nakanishi, T. Kinoshita, T. Tada, T. Fujita, H. Hatanaka, A. Sato

        9   2397 - 2402   1999.06

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  • Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist Reviewed

    S. Kuroda, A. Akahane, H. Itani, S. Nishimura, K. Durkin, T. Kinoshita, Y. Tenda, K. Sakane

    Bioorg. Med. Chem. Lett.   9   1979 - 1984   1999.04

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  • Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5alfa]pyridin-3-yl)-1(6H)-pyridazine-butanoic acid (FK838) : A novel non-xanthine adenosine A1 receptor antagonist with potent diruretic activity Reviewed

    A. Akahane, H. Katayama, T. Mitsunaga, T. Kato, T. Kinoshita, Y. Kita, T. Kusunoki T. Terai, K. Yoshida, Y. Shiokawa

    J. Med. Chem.   42   779 - 783   1999.04

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  • Complexation of C60 with hexahomooxacalix[3]arenes and supramolecular structures of complexes in the solid state Reviewed

    K. Tsubaki, K. Tanaka, T. Kinoshita, K. Fuji

    Chem. Commun.   895 - 896   1998.12

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  • Palladium-catalyzed asymmetric reduction of allylic esters with a new chiral monodentate ligand, 8-diphenylphosphino-8'-mothoxy-1,1'-binaphthyl Reviewed

    K. Fuji, M. Sakurai, T. Kinoshita, T. Kawabata

    Tetrahedron Lett.   39   6323 - 6326   1998.12

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  • Stepwise construction of some hexahomooxacalix[3]arenes and their comformations in solid state Reviewed

    K. Tsubaki, T. Otsubo, K. Tanaka, K. Fuji, T. Kinoshita

    J. Org. Chem.   63   3260 - 3265   1998.05

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  • The first synthesis of an optically active molecular bevel gear with only two cogs on each wheel Reviewed

    The first synthesis of an optically active molecular bevel gear with only two cogs on each wheel

    Tetrahedron Lett.   39   1373 - 1376   1998.03

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  • Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA: cholesterol O-acyltransferase (ACAT) bearing a pyrazol ring Reviewed

    A. Tanaka, T. Terasawa, H. Hagihara, T. Kinoshita, Y. Sakuma, N. Ishibe, M. Sawada, H. Takasugi, H. Tanaka

    Bioorg. Med. Chem. Lett.   8   81 - 86   1998.01

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  • Assessment of the activity of 8-diphenylphoosphosphino-8'-mothoxy-1,1'-binaphthyl as a ligand for palladium-catalyzed reactions Reviewed

    K. Fuji, M. Sakurai, T. Kinoshita, T. Tada, A. Kuroda, T. Kawabata

    Chem. Pharm. Bull.   45   1524 - 1526   1997.10

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  • Structure of the zinc endoprotease from Streptomyces caespitosus Reviewed

    G. Kurisu, T. Kinoshita, A. Sugimoto, A. Nagara, Y. Kai, N. Kasai, S. Harada

    J. Biochem.   121   304 - 308   1997.02

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  • Unexpectically facile racemization of 8-diphenylphosphinoyl-8'-methoxy-1.1'-binaphthyl Reviewed

    K. Fuji, M. Sakurai, N. Tohkai, A. Kuroda, T. Kawabata, Y. Fukazawa, T. Kinoshita, T. Tada

    Chem. Commun.   1609 - 1610   1996.12

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  • A novel [3+2] annulation: synthesis and X-ray crystallographic structure of a novel tetrahydropyrazolo[1,5-a]quinoline, an intermediate towards new tricyclic quinolone antibacterials Reviewed

    D. Barrett, H. Sasaki, T. Kinoshita, K. Sakane

    Chem. Commun.   61 - 62   1996.12

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  • A novel synthesis of the pyrazolo[1,5-a]quinoline ring system. New N1-C2 bridged DNA gyrase inhibitors via a novel tandem 1,4-conjugate addition-Michael [3+2] annulation process Reviewed

    D. Barrett, H. Sasaki, T. Kinoshita, A. Fujikawa, K. Sakane

    Tetrahedron   52   8471 - 8488   1996.10

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  • Alkylation of 1-[N-(hydroxymethyl)-N-methylamino]-4-quinolones. An improved preparation of intermediates for novel potent tricyclic quinolone antibacterial agents Reviewed

    D. Barrett, H. Sasaki, H. Tsutsumi, T. Kinoshita, K. Sakane

    Bull. Chem. Soc. Jpn   69   1371 - 1376   1996.09

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  • Studies on Cerebral Protective Agents. X. Synthesis and evaluation of anticonvulsant activities for novel 4,5,6,7-tetrahydrothieno[3,3-c]pyridines and related compounds Reviewed

    M. Ohkubo, A. Kuno, K. Katsuta, Y. Ueda, K. Shirakawa, H. Nakanishi, T. Kinoshita, H. Takasugi

    Chem. Pharm. Bull.   44   778 - 784   1996.06

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  • Studies on cerebral protective agents. IX. Synthesis of novel 1,2,3,4-tetrahydroisoquinolines as N-Methyl-D-aspartate antagonists Reviewed

    M. Ohkubo, A. Kuno, K. Kathuta, Y. Ueda, K. Shirakawa, H. Nakanishi, I. Nakanishi, T. Kinoshita, H. Takasugi

    Chem. Pharm. Bull.   44   95 - 102   1996.01

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  • Synthesis of new 1,8-bridged tricyclic quinolones by a novel intramolecular arylation of N-1 tethered malonamides Reviewed

    D. Barrett, H. Tsutsumi, T. Kinoshita, M. Murata, K. Sakan

    Tetrahedron   51   11125 - 11140   1995.10

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  • Asymmetric synthesis of FR165914: a novel ?3-adrenergic agonist with a benzocycloheptane structure Reviewed

    K. Hattori, M. Nagano, T. Kato, I. Nakanishi, K. Imai, T. Kinoshita, K. Sakane

    Bioorg. Med. Chem. Lett.   5   2821 - 2823   1995.06

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  • Complete amino acid sequence of a zinc matalloendoprotease from Streptomyces caespitosus Reviewed

    S. Harada, T. Kinoshita, N. Kasai, S., Tsunasawa, F. Sakiyama

    Eur. J. Biochem.   233   683 - 686   1995.04

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  • Studies on a novel, potent and orally effective cheolecytokinin. An antagonist, FK-480. Synthesis and structure-activity relationships of FK-480 and related compounds Reviewed

    Y. Sato, T. Matsuo, H. Sogabe, H. Itoh, T. Tada, T. Kinoshita, K. Yoshida, T. Takaya

    Chem. Pharm. Bull.   42   2071 - 2083   1994.06

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  • Crystallization and main-chain structure of neutral protease from Streptomyces caespitosus Reviewed

    S. Harada, K.Kitadokoro, T. Kinoshita, Y. Kai, N.Kasai

    J. Biochem.   110   46 - 49   1991.01

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    Kind of work:Joint Work  

▼display all

Books and Other Publications

  • Protein allostery in drug design

    Takayoshi Kinoshita( Role: Joint author)

    Springer-Nature  2019.07 

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    Responsible for pages:45-64  

  • バイオサイエンス実験 入門から応用へ

    木下誉富( Role: Joint author)

    大阪府立大学共同出版会  2016.03 

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    Responsible for pages:17-24, 109-116  

  • 次世代がん戦略研究 update がん基礎生物学 革新的シーズ育成に向けて

    足立恵理、酒井克也、木下誉富、松本邦夫( Role: Joint author)

    南山堂  2013.10 

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    Responsible for pages:118-125  

  • タンパク質結晶の新展開-新しい育成技術から構造解析・応用研究へ-<普及版>

    木下誉富( Role: Joint author)

    シーエムシー出版  2013.10 

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    Responsible for pages:205-214  

  • 社会との垣根を超える大学の挑戦

    藤井郁雄、円谷健、藤原大佑、多田俊治、木下誉富、恩田真紀、切畑光統、谷森紳治、神川憲、乾隆( Role: Joint author)

    (株)エヌ・ティー・エス  2011.12 

  • 創薬研究のストラテジー

    木下誉富( Role: Joint author)

    金芳堂  2011.03 

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    Responsible for pages:83-89  

  • コンピューターで薬を創ろう

    木下誉富、仲西功( Role: Joint author)

    ケイ・ディーネオブック  2009.06 

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    Responsible for pages:81-94  

  • タンパク質結晶の新展開-新しい育成技術から構造解析・応用研究へ-

    木下誉富( Role: Joint author)

    シーエムシー出版  2008.05 

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    Responsible for pages:205-214  

▼display all

Presentations

  • Protein kinase CK2阻害活性を有するプリン誘導体の構造活性相関研究—プリン環2位への種々の飽和炭化水素置換基の導入— Domestic conference

    中谷汐里、中川愛理、吉岡賢司、西脇敬二、中村真也、露口正人、木下誉富、仲西功

    日本薬学会第144年会  2024.03  日本薬学会

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    Presentation type:Poster presentation  

    Venue:横浜  

  • クライオ電子顕微鏡を用いたMAP2K6-p38αMAPK複合体の構造研究 Domestic conference

    川端凌弥、宮園真吾、木下誉富

    BioMedical Forum 2024  2023.12  大阪公立大学研究推進機構

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    Presentation type:Poster presentation  

    Venue:堺  

  • In-crystal化合物交換法によるMAP2K4-阻害剤複合体結晶の調製 Domestic conference

    山下直之、祐村清悟、木下誉富

    BioMedical Forum 2024  2023.12  大阪公立大学研究推進機構

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    Presentation type:Poster presentation  

    Venue:堺  

  • プロテインキナーゼCK2αの結晶水を考慮した阻害剤の設計と合成および活性評価 Domestic conference

    西脇敬二、中谷汐里、中村真也、吉岡賢司、中川愛理、露口正人、木下誉富、仲西功

    40回メディシナルケミストリーシンポジウム  2023.11  日本薬学会医薬化学部会

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    Presentation type:Poster presentation  

    Venue:名古屋  

  • Intact and phosphorylated peptides derived from the N- and C-terminal regions enhance and inhibit cMet kinase activity, respectively Domestic conference

    2023.11 

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    Presentation type:Poster presentation  

  • Mechanism-based Discovery of peptide inhibitors of FGFR3/G697C, a pathogenic active mutant Domestic conference

    2023.11 

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    Presentation type:Poster presentation  

  • p38αMAPK による基質Smad3の認識機構の解明 Domestic conference

    長谷川誠将、永尾春菜、澤匡明、木下誉富

    令和5年度日本結晶学会年会  2023.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:宇部  

  • In-crystal 交換法によるMAP2K4-阻害剤複合体結晶の調製 Domestic conference

    山下直之、祐村清悟、木下誉富

    令和5年度日本結晶学会年会  2023.10 

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    Presentation type:Poster presentation  

  • MAXS reveals a disorder-to-order transition of the intrinsically disordered region in active MAP2K6 Domestic conference

    2023.10 

  • Insight into the Binding Modes of Allosteric ERK2 Inhibitors using Metadynamics Simulations Domestic conference

    2023.10 

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    Presentation type:Poster presentation  

  • Conserved gatekeeper methionine determines the accessibility to the ATP-sites and selectivity among MAP2K1/4/7 Domestic conference

    2023.10 

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    Presentation type:Poster presentation  

  • Steps forward beyond the crystal structures: MAXS reveals the potential massive movements during the catalytic action of a kinase International conference

    T. Matsumoto, A. Yamano, Y. Murakawa, H. Fukada, M. Sawa, T. Kinoshita

    26th Congress and General Assembly of the International Union of Crystallography IUCr2023  2023.08  International Union of Crystallography

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    Presentation type:Poster presentation  

    Venue:Melbourne  

  • MAP2K4-阻害剤複合体のX線結晶構造-共有結合できない共有結合性阻害剤- Domestic conference

    祐村清悟、山下直之、北川大輔、澤匡明、木下誉富

    第23回日本蛋白質科学会年会  2023.07  日本蛋白質科学会

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    Presentation type:Poster presentation  

    Venue:名古屋  

  • Protein Kinase CK2阻害活性を有するプリン誘導体の構造活性相関研究―結合ポケット奥の結晶水を残すCK2阻害剤設計― Domestic conference

    中谷汐里、中川愛理、吉岡賢司、西脇敬二、中村真也、露口正人、木下誉富、仲西功

    日本薬学会第143年会  2023.03  日本薬学会

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    Presentation type:Poster presentation  

    Venue:札幌  

  • アミノピラゾール系阻害剤の二つの結合様式が示すCK2α1選択的阻害剤への手掛かり Domestic conference

    露口正人、池田朝香、北川大輔、澤匡明、中村真也、仲西功、木下誉富

    2022年度量子ビームサイエンスフェスタ(第14回MLFシンポジウム/第40回PFシンポジウム)  2023.03 

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    Presentation type:Poster presentation  

    Venue:つくば  

  • MAP2K4/5Z7-oxozeaenol複合体のX線結晶構造解析 Domestic conference

    祐村清悟、山下直之、木下誉富

    BioMedical Forum 2023  2023.01 

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    Presentation type:Poster presentation  

    Venue:大阪  

  • 二価性阻害剤の結合様式が示す特異的CK2α1阻害剤の創出基盤 Domestic conference

    池田朝香、露口正人、北川大輔、澤匡明、中村真也、西脇敬二、仲西功、木下誉富

    BioMedical Forum 2023  2023.01 

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    Presentation type:Poster presentation  

    Venue:大阪  

  • 高選択性p38α阻害剤創出に向けた構造基盤 Domestic conference

    長谷川誠将、吉田茉由、杉山肇、木下誉富

    BioMedical Forum 2023  2023.01 

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    Presentation type:Poster presentation  

    Venue:大阪  

  • MAP2K4-共有結合性阻害剤のX線結晶構造解析 Domestic conference

    祐村清悟、山下直之、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • セリン・スレオニンキナーゼMosの活性制御機構の解明 Domestic conference

    馬場健吉、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • FGFR3/G697Cの触媒機構の解明に向けた構造生物学研究 Domestic conference

    鈴木大輔、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • MAP2K4阻害剤の相互作用様式の解明 Domestic conference

    山下直之、祐村清悟、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • 高選択性MAPキナーゼ阻害剤創出に向けた構造基盤 Domestic conference

    長谷川誠将、吉田茉由、杉山肇、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • 昆虫由来のプロテインキナーゼの構造生物学的研究 Domestic conference

    池田朝香、井戸邦夫、木下誉富

    令和4年度日本結晶学会年会  2022.10  日本結晶学会

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    Presentation type:Poster presentation  

    Venue:兵庫  

  • Insight into Allosteric ERK2 Inhibitors by using Metadynamics Simulations Domestic conference

    2022.10 

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    Presentation type:Poster presentation  

  • Protein Kinase CK2阻害活性を有するプリン誘導体の構造活性相関研究―環式飽和炭化水素置換基の導入― Domestic conference

    中谷汐里、西脇敬二、中村真也、露口正人、木下誉富、仲西功

    第72回日本薬学会関西支部大会  2022.10  日本薬学会関西支部

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    Presentation type:Poster presentation  

    Venue:大阪  

  • MAXS reveals the conformational changes of intrinsically disordered region of MAP2K6 International conference

    T. Matsumoto, S. Hasegawa, T. Hasegawa, T. Kinoshita

    33th European Crystallographic Meeting  2022.08  European Crystallographic Association

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    Presentation type:Poster presentation  

  • MAXSを活用した蛋白質の構造変化と機能の関係に基づく創薬戦略

    松本 崇, 山野 昭人, 村川 優花, 深田 はるみ, 澤 匡明, 木下 誉富

    日本農薬学会大会講演要旨集  2022.03  日本農薬学会

  • インシリコスクリーニングから得たアロステリック阻害剤の選択性に関する考察 Domestic conference

    吉田茉由、杉山肇、永尾春菜、澤匡明、木下誉富

    第49回構造活性相関シンポジウム  2021.11  日本薬学会

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    Presentation type:Poster presentation  

  • CK2a1選択性向上に向けたアロステリック部位の構造知見 Domestic conference

    池田朝香、露口正人、中村真也、西脇敬二、仲西功、木下誉富

    第49回構造活性相関シンポジウム  2021.11  日本薬学会

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    Presentation type:Poster presentation  

  • 高選択性MAP2K阻害剤の開発に向けた構造基盤の構築 Domestic conference

    祐村清悟、木下誉富

    令和3年(2021年)度日本結晶学会年会  2021.11  日本結晶学会

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    Presentation type:Poster presentation  

  • MAP2K3の非twin結晶の取得に向けた結晶化検討 Domestic conference

    中野可鈴、村川優花、木下誉富

    令和3年(2021年)度日本結晶学会年会  2021.11  日本結晶学会

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    Presentation type:Poster presentation  

  • 構造生物学を基盤としたキナーゼ創薬研究 Invited Domestic conference

    木下誉富

    第35回農薬デザイン研究会  2021.11  日本農薬学会

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    Presentation type:Oral presentation (invited, special)  

  • Evaluation of the peptide derived from the N- and C-terminal regions of kinase domain for allosteric control of receptor tyrosine kinase cMet Domestic conference

    田中友輝、松本邦夫、木下誉富

    第58回ペプチド討論会  2021.10  日本ペプチド学会

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    Presentation type:Poster presentation  

  • Molecular basis of allosteric ERK2 inhibitors discovered by in silico screening Domestic conference

    吉田茉由、杉山肇、永尾春菜、澤匡明、木下誉富

    CBI学会2021年大会  2021.10  CBI学会

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    Presentation type:Poster presentation  

  • Insight into allosteric ERK2 inhibitors by using fragment molecular orbital method Domestic conference

    杉山肇、吉田茉由、木下誉富

    CBI学会2021年大会  2021.10  CBI学会

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    Presentation type:Poster presentation  

  • 中性子線結晶構造解析とMDシミュレーションを駆使した酵素反応の理解 Invited Domestic conference

    木下誉富

    CBI学会2021年大会スポンサーセッション新世代中性子構造生物学研究会  2021.10  CBI学会

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    Presentation type:Oral presentation (invited, special)  

  • 高選択的CK2a1阻害剤の創出を目指したニトリル系化合物の阻害機構の解明 Domestic conference

    池田朝香、露口正人、中村真也、西脇敬二、仲西功、木下誉富

    第21回日本蛋白質科学会年会  2021.06  日本蛋白質科学会

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    Presentation type:Poster presentation  

  • KIMサイト結合型ERK2キナーゼ阻害剤の作用機序の解明 Domestic conference

    吉田茉由、森悠里花、永尾春菜、澤匡明、木下誉富

    第21回日本蛋白質科学会年会  2021.06  日本蛋白質科学会

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    Presentation type:Poster presentation  

  • プリン骨格を有するCK2阻害剤の構造活性相関研究 プリン骨格の互変異性の検討

    河津 有貴, 中川 愛理, 吉岡 賢司, 中村 真也, 西脇 敬二, 露口 正人, 木下 誉富, 仲西 功

    日本薬学会年会要旨集  2020.03  (公社)日本薬学会

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Outline of collaborative research (seeds)

  • キナーゼの生化学実験

  • キナーゼのX線結晶構造解析

Charge of on-campus class subject

  • 生物化学実験2

    2024   Weekly class   Undergraduate

  • 構造生物学

    2024   Weekly class   Undergraduate

  • 基礎物理化学

    2024   Weekly class   Undergraduate

  • 基礎物理化学

    2024   Weekly class   Undergraduate

  • 生物化学特別講義D

    2024   Intensive lecture   Graduate school

  • 構造生物学特論

    2024   Weekly class   Graduate school

  • 生物化学特別研究2A

    2024   Intensive lecture   Graduate school

  • 生物化学特別研究1A

    2024   Intensive lecture   Graduate school

  • 生物化学特別演習2A

    2024   Intensive lecture   Graduate school

  • 生物化学特別演習1A

    2024   Intensive lecture   Graduate school

  • 生物化学特別講義H

    2024   Intensive lecture   Graduate school

  • 生物化学特別研究5A

    2024   Intensive lecture   Graduate school

  • 生物化学特別研究4A

    2024   Intensive lecture   Graduate school

  • 生物化学特別研究3A

    2024   Intensive lecture   Graduate school

  • 生物化学特別演習5A

    2024   Intensive lecture   Graduate school

  • 生物化学特別演習4A

    2024   Intensive lecture   Graduate school

  • 生物化学特別演習3A

    2024   Intensive lecture   Graduate school

  • 創薬科学実習2

    2024   Intensive lecture   Undergraduate

  • 創薬科学実習1

    2024   Intensive lecture   Undergraduate

  • 創薬科学のすすめ

    2024   Weekly class   Graduate school

  • 創薬科学のすすめ

    2024   Weekly class   Graduate school

  • 生物化学への招待

    2024   Weekly class   Graduate school

  • 構造生物学

    2024   Weekly class   Undergraduate

  • 基礎物理化学

    2024   Weekly class   Undergraduate

  • 研究企画ゼミナール1

    2023   Intensive lecture   Graduate school

  • 創薬科学のすすめ

    2023   Weekly class   Graduate school

  • 生物化学への招待

    2023   Weekly class   Graduate school

  • 生物化学特別研究4A

    2023   Intensive lecture   Graduate school

  • 生物化学特別研究3A

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習4A

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習3A

    2023   Intensive lecture   Graduate school

  • 研究企画ゼミナール2

    2023   Intensive lecture   Graduate school

  • 構造生物学特論

    2023   Weekly class   Graduate school

  • 生物化学特別研究2A

    2023   Intensive lecture   Graduate school

  • 生物化学特別研究1A

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習2A

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習1A

    2023   Intensive lecture   Graduate school

  • 研究企画ゼミナール1

    2023   Intensive lecture   Graduate school

  • 創薬科学実習II

    2023   Intensive lecture   Undergraduate

  • 創薬科学実習I

    2023   Intensive lecture   Undergraduate

  • 構造生物学

    2023   Weekly class   Undergraduate

  • 基礎物理化学

    2023   Weekly class   Undergraduate

  • 生物科学実験II

    2023   Weekly class   Undergraduate

  • 生物化学実験1

    2023   Weekly class   Undergraduate

  • 生化学2

    2023   Weekly class   Undergraduate

  • 生物化学概論

    2023   Weekly class   Undergraduate

  • 生物系機器分析学

    2023   Weekly class   Undergraduate

  • 生物化学特別研究4B

    2023   Intensive lecture   Graduate school

  • 生物化学特別研究3B

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習4B

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習3B

    2023   Intensive lecture   Graduate school

  • 研究企画ゼミナール2

    2023   Intensive lecture   Graduate school

  • 生物化学特別研究2B

    2023   Intensive lecture   Graduate school

  • 生物化学特別研究1B

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習2B

    2023   Intensive lecture   Graduate school

  • 生物化学特別演習1B

    2023   Intensive lecture   Graduate school

  • Laboratory Training in Drug Discovery Sciences & Technology II

    2021   Practical Training  

  • Laboratory Training in Drug Discovery Sciences & Technology I

    2021   Practical Training  

  • Experiment in Biological Science II

    2021   Practical Training  

  • Instrumental Analysis in Biology

    2021    

  • Introduction of Drug Discovery

    2021    

  • English for Scientists

    2021    

  • Structural Biology

    2021    

  • Fundamental Physical Chemistry

    2021    

  • Structural Biology

    2021    

▼display all

Number of papers published by graduate students

  • 2023

    Number of undergraduate student / college student presentations:Number of graduate students presentations:3

Number of instructed thesis, researches

  • 2023

    Number of instructed the graduation thesis:Number of graduation thesis reviews:3

    [Number of instructed the Master's Program] (previous term):[Number of instructed the Master's Program] (letter term):1

    [Number of master's thesis reviews] (chief):[Number of master's thesis reviews] (vice-chief):5

    [Number of doctoral thesis reviews] (chief):[Number of doctoral thesis reviews] (vice-chief):1

  • 2022

    Number of instructed the graduation thesis:Number of graduation thesis reviews:4

    [Number of instructed the Master's Program] (previous term):[Number of instructed the Master's Program] (letter term):1

    [Number of master's thesis reviews] (chief):[Number of master's thesis reviews] (vice-chief):6

  • 2021

    Number of instructed the graduation thesis:Number of graduation thesis reviews:3

    [Number of instructed the Master's Program] (previous term):

    [Number of master's thesis reviews] (chief):[Number of master's thesis reviews] (vice-chief):4

    [Number of doctoral thesis reviews] (vice-chief):3

  • 2020

    Number of instructed the graduation thesis:

  • 2019

    Number of instructed the graduation thesis:

Academic Activities

  • European Journal of Medicinal Chemistry

    Role(s): Peer review

    2024.02

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    Type:Peer review 

  • Bioorganic and Medicinal Chemistry Letters

    Role(s): Peer review

    2024.02

     More details

    Type:Peer review 

  • Bioorganic and Medicinal Chemistry Letters

    Role(s): Peer review

    2024.01

     More details

    Type:Peer review 

  • Bioorganic Chemistry

    Role(s): Peer review

    2023.12

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    Type:Peer review 

  • Heliyon

    Role(s): Peer review

    2023.11

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    Type:Peer review 

  • European Journal of Medicinal Chemistry

    Role(s): Peer review

    2023.09

     More details

    Type:Peer review 

  • Bioorganic and Medicinal Chemistry Letters

    Role(s): Peer review

    2023.07

     More details

    Type:Peer review 

  • Bioorganic and Medicinal Chemistry Letters

    Role(s): Peer review

    2023.07

     More details

    Type:Peer review 

  • European Journal of Medicinal Chemistry

    Role(s): Peer review

    2023.05

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    Type:Peer review 

  • Acta Crystallographica Section D

    Role(s): Peer review

    2023.05

     More details

    Type:Peer review 

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Original item・Special report (Social Activity)

  • 2023

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    SDGs:

    Original item:兵庫県立尼崎小田高等学校「大阪公立大学研修」講師

Foreigner acceptance

  • 2023

    International Students :1