Literature DB >> 15482920

Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.

Hongyu Zhao1, Gang Liu, Zhili Xin, Michael D Serby, Zhonghua Pei, Bruce G Szczepankiewicz, Philip J Hajduk, Cele Abad-Zapatero, Charles W Hutchins, Thomas H Lubben, Stephen J Ballaron, Deanna L Haasch, Wiweka Kaszubska, Cristina M Rondinone, James M Trevillyan, Michael R Jirousek.   

Abstract

Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.

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Year:  2004        PMID： 15482920     DOI： 10.1016/j.bmcl.2004.08.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

1.  A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH.

Authors:  Fa Liu; Ramin Mollaaghababa Hakami; Beverly Dyas; Medhanit Bahta; George T Lountos; David S Waugh; Robert G Ulrich; Terrence R Burke
Journal:  Bioorg Med Chem Lett       Date:  2010-03-15       Impact factor: 2.823

2.  Discovery of inhibitors targeting protein tyrosine phosphatase 1B using a combined virtual screening approach.

Authors:  Dan Zhao; Lu Sun; Shijun Zhong
Journal:  Mol Divers       Date:  2021-10-16       Impact factor: 3.364

3.  Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.

Authors:  Ying-Nan P Chen; Matthew J LaMarche; Ho Man Chan; Peter Fekkes; Jorge Garcia-Fortanet; Michael G Acker; Brandon Antonakos; Christine Hiu-Tung Chen; Zhouliang Chen; Vesselina G Cooke; Jason R Dobson; Zhan Deng; Feng Fei; Brant Firestone; Michelle Fodor; Cary Fridrich; Hui Gao; Denise Grunenfelder; Huai-Xiang Hao; Jaison Jacob; Samuel Ho; Kathy Hsiao; Zhao B Kang; Rajesh Karki; Mitsunori Kato; Jay Larrow; Laura R La Bonte; Francois Lenoir; Gang Liu; Shumei Liu; Dyuti Majumdar; Matthew J Meyer; Mark Palermo; Lawrence Perez; Minying Pu; Edmund Price; Christopher Quinn; Subarna Shakya; Michael D Shultz; Joanna Slisz; Kavitha Venkatesan; Ping Wang; Markus Warmuth; Sarah Williams; Guizhi Yang; Jing Yuan; Ji-Hu Zhang; Ping Zhu; Timothy Ramsey; Nicholas J Keen; William R Sellers; Travis Stams; Pascal D Fortin
Journal:  Nature       Date:  2016-06-29       Impact factor: 49.962

4.  Synthesis and Biological Evaluation of Novel N-phenyl-5-carboxamidyl Isoxazoles as Potential Chemotherapeutic Agents for Colon Cancer.

Authors:  Jiajiu Shaw; Ben Chen; Jean P Bourgault; Hao Jiang; Narendra Kumar; Jayshree Mishra; Frederick A Valeriote; Joe Media; Kevin Bobbitt; Halina Pietraszkiewicz; Matthew Edelstein; Peter R Andreana
Journal:  Am J Biomed Sci       Date:  2012

5.  Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.

Authors:  Alan P Kozikowski; Subhasish Tapadar; Doris N Luchini; Ki Hwan Kim; Daniel D Billadeau
Journal:  J Med Chem       Date:  2008-07-22       Impact factor: 7.446

6.  Novel Mixed-Type Inhibitors of Protein Tyrosine Phosphatase 1B. Kinetic and Computational Studies.

Authors:  Marie Jazmín Sarabia-Sánchez; Pedro Josué Trejo-Soto; José Miguel Velázquez-López; Carlos Carvente-García; Rafael Castillo; Alicia Hernández-Campos; Claudia Avitia-Domínguez; Daniel Enríquez-Mendiola; Erick Sierra-Campos; Mónica Valdez-Solana; José Manuel Salas-Pacheco; Alfredo Téllez-Valencia
Journal:  Molecules       Date:  2017-12-20       Impact factor: 4.411

7.  A New Paradigm for KIM-PTP Drug Discovery: Identification of Allosteric Sites with Potential for Selective Inhibition Using Virtual Screening and LEI Analysis.

Authors:  James Adams; Benjamin P Thornton; Lydia Tabernero
Journal:  Int J Mol Sci       Date:  2021-11-11       Impact factor: 5.923

8.  QSAR Study on a Series of Protein Tyrosine Phosphatase 1B Inhibitors.

Authors:  Rajendra S Mehta; Hetal R Prajapati; Dinesh V Thakkar; Pathik S Brahmkshatriya
Journal:  Int J Biomed Sci       Date:  2008-12
  8 in total

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