Literature DB >> 26819674

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Marian C Bryan1, Daniel J Burdick1, Bryan K Chan1, Yuan Chen1, Saundra Clausen1, Jennafer Dotson1, Charles Eigenbrot1, Richard Elliott2, Emily J Hanan1, Robert Heald2, Philip Jackson2, Hank La1, Michael Lainchbury2, Shiva Malek1, Sam E Mann2, Hans E Purkey1, Gabriele Schaefer1, Stephen Schmidt1, Eileen Seward2, Steve Sideris1, Shumei Wang1, Ivana Yen1, Christine Yu1, Timothy P Heffron1.   

Abstract

The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.

Entities:  

Keywords:  Mutant EGFR; T790M; noncovalent; pyridone

Year:  2015        PMID： 26819674      PMCID： PMC4716594          DOI： 10.1021/acsmedchemlett.5b00428

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  15 in total

1.  Effects of oncogenic mutations on the conformational free-energy landscape of EGFR kinase.

Authors:  Ludovico Sutto; Francesco Luigi Gervasio
Journal:  Proc Natl Acad Sci U S A       Date:  2013-06-10       Impact factor: 11.205

2.  EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors.

Authors:  Dalia Ercan; Hwan Geun Choi; Cai-Hong Yun; Marzia Capelletti; Ting Xie; Michael J Eck; Nathanael S Gray; Pasi A Jänne
Journal:  Clin Cancer Res       Date:  2015-05-06       Impact factor: 12.531

3.  Structural Differences between Wild-Type and Double Mutant EGFR Modulated by Third-Generation Kinase Inhibitors.

Authors:  Melissa A Lowder; Amy E Doerner; Alanna Schepartz
Journal:  J Am Chem Soc       Date:  2015-05-14       Impact factor: 15.419

Review 4.  The role of ligand efficiency metrics in drug discovery.

Authors:  Andrew L Hopkins; György M Keserü; Paul D Leeson; David C Rees; Charles H Reynolds
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

Review 5.  Mechanisms of cutaneous toxicities to EGFR inhibitors.

Authors:  Mario E Lacouture
Journal:  Nat Rev Cancer       Date:  2006-10       Impact factor: 60.716

Review 6.  Epidermal growth factor receptor mutations in lung cancer.

Authors:  Sreenath V Sharma; Daphne W Bell; Jeffrey Settleman; Daniel A Haber
Journal:  Nat Rev Cancer       Date:  2007-03       Impact factor: 60.716

7.  Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways.

Authors:  Raffaella Sordella; Daphne W Bell; Daniel A Haber; Jeffrey Settleman
Journal:  Science       Date:  2004-07-29       Impact factor: 47.728

8.  Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

Authors:  Annette O Walter; Robert Tjin Tham Sjin; Henry J Haringsma; Kadoaki Ohashi; Jing Sun; Kwangho Lee; Aleksandr Dubrovskiy; Matthew Labenski; Zhendong Zhu; Zhigang Wang; Michael Sheets; Thia St Martin; Russell Karp; Dan van Kalken; Prasoon Chaturvedi; Deqiang Niu; Mariana Nacht; Russell C Petter; William Westlin; Kevin Lin; Sarah Jaw-Tsai; Mitch Raponi; Terry Van Dyke; Jeff Etter; Zoe Weaver; William Pao; Juswinder Singh; Andrew D Simmons; Thomas C Harding; Andrew Allen
Journal:  Cancer Discov       Date:  2013-09-24       Impact factor: 39.397

9.  Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor.

Authors:  Jennifer Stamos; Mark X Sliwkowski; Charles Eigenbrot
Journal:  J Biol Chem       Date:  2002-08-23       Impact factor: 5.157

10.  Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.

Authors:  Emily J Hanan; Charles Eigenbrot; Marian C Bryan; Daniel J Burdick; Bryan K Chan; Yuan Chen; Jennafer Dotson; Robert A Heald; Philip S Jackson; Hank La; Michael D Lainchbury; Shiva Malek; Hans E Purkey; Gabriele Schaefer; Stephen Schmidt; Eileen M Seward; Steve Sideris; Christine Tam; Shumei Wang; Siew Kuen Yeap; Ivana Yen; Jianping Yin; Christine Yu; Inna Zilberleyb; Timothy P Heffron
Journal:  J Med Chem       Date:  2014-11-20       Impact factor: 7.446
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  3 in total

1.  Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers.

Authors:  Caolin Wang; Shan Xu; Liang Peng; Bingliang Zhang; Hong Zhang; Yingying Hu; Pengwu Zheng; Wufu Zhu
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

2.  How Far Are We from the Rapid Prediction of Drug Resistance Arising Due to Kinase Mutations?

Authors:  Mehmet Erguven; Tülay Karakulak; M Kasim Diril; Ezgi Karaca
Journal:  ACS Omega       Date:  2021-01-04

3.  Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors.

Authors:  Yuanbiao Tu; Caolin Wang; Zunhua Yang; Bingbing Zhao; Luogen Lai; Qi Yang; Pengwu Zheng; Wufu Zhu
Journal:  Comput Struct Biotechnol J       Date:  2018-10-30       Impact factor: 7.271
  3 in total

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