Literature DB >> 22819762

Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

Hwan Geun Choi1, Jianming Zhang, Ellen Weisberg, James D Griffin, Taebo Sim, Nathanael S Gray.   

Abstract

HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I- Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22819762      PMCID： PMC3415686          DOI： 10.1016/j.bmcl.2012.06.036

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


  17 in total

1.  In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells.

Authors:  Miriam Puttini; Addolorata Maria Luce Coluccia; Frank Boschelli; Loredana Cleris; Edoardo Marchesi; Arianna Donella-Deana; Shaheen Ahmed; Sara Redaelli; Rocco Piazza; Vera Magistroni; Federica Andreoni; Leonardo Scapozza; Franca Formelli; Carlo Gambacorti-Passerini
Journal:  Cancer Res       Date:  2006-11-17       Impact factor: 12.701

2.  An efficient rapid system for profiling the cellular activities of molecular libraries.

Authors:  Jonathan S Melnick; Jeff Janes; Sungjoon Kim; Jim Y Chang; Daniel G Sipes; Drew Gunderson; Laura Jarnes; Jason T Matzen; Michael E Garcia; Tami L Hood; Ronak Beigi; Gang Xia; Richard A Harig; Hayk Asatryan; S Frank Yan; Yingyao Zhou; Xiang-Ju Gu; Alham Saadat; Vicki Zhou; Frederick J King; Christopher M Shaw; Andrew I Su; Robert Downs; Nathanael S Gray; Peter G Schultz; Markus Warmuth; Jeremy S Caldwell
Journal:  Proc Natl Acad Sci U S A       Date:  2006-02-21       Impact factor: 11.205

3.  A general strategy for creating "inactive-conformation" abl inhibitors.

Authors:  Barun Okram; Advait Nagle; Francisco J Adrián; Christian Lee; Pingda Ren; Xia Wang; Taebo Sim; Yongping Xie; Xing Wang; Gang Xia; Glen Spraggon; Markus Warmuth; Yi Liu; Nathanael S Gray
Journal:  Chem Biol       Date:  2006-07

4.  Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome.

Authors:  B J Druker; C L Sawyers; H Kantarjian; D J Resta; S F Reese; J M Ford; R Capdeville; M Talpaz
Journal:  N Engl J Med       Date:  2001-04-05       Impact factor: 91.245

5.  Overriding imatinib resistance with a novel ABL kinase inhibitor.

Authors:  Neil P Shah; Chris Tran; Francis Y Lee; Ping Chen; Derek Norris; Charles L Sawyers
Journal:  Science       Date:  2004-07-16       Impact factor: 47.728

6.  The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.

Authors:  Mark T Bilodeau; Leonard D Rodman; Georgia B McGaughey; Kathleen E Coll; Timothy J Koester; William F Hoffman; Randall W Hungate; Richard L Kendall; Rosemary C McFall; Keith W Rickert; Ruth Z Rutledge; Kenneth A Thomas
Journal:  Bioorg Med Chem Lett       Date:  2004-06-07       Impact factor: 2.823

7.  Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells.

Authors:  B J Druker; S Tamura; E Buchdunger; S Ohno; G M Segal; S Fanning; J Zimmermann; N B Lydon
Journal:  Nat Med       Date:  1996-05       Impact factor: 53.440

8.  Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

Authors:  Ellen Weisberg; Paul W Manley; Werner Breitenstein; Josef Brüggen; Sandra W Cowan-Jacob; Arghya Ray; Brian Huntly; Doriano Fabbro; Gabriele Fendrich; Elizabeth Hall-Meyers; Andrew L Kung; Jürgen Mestan; George Q Daley; Linda Callahan; Laurie Catley; Cara Cavazza; Mohammad Azam; Azam Mohammed; Donna Neuberg; Renee D Wright; D Gary Gilliland; James D Griffin
Journal:  Cancer Cell       Date:  2005-02       Impact factor: 31.743

Review 9.  AMN107: tightening the grip of imatinib.

Authors:  Thomas O'Hare; Denise K Walters; Michael W N Deininger; Brian J Druker
Journal:  Cancer Cell       Date:  2005-02       Impact factor: 31.743

10.  Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations.

Authors:  Markus A Seeliger; Pratistha Ranjitkar; Corynn Kasap; Yibing Shan; David E Shaw; Neil P Shah; John Kuriyan; Dustin J Maly
Journal:  Cancer Res       Date:  2009-03-10       Impact factor: 12.701
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  2 in total

1.  The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity.

Authors:  Soumya Ray; Samantha Bender; Stephanie Kang; Regina Lin; Marcie A Glicksman; Min Liu
Journal:  J Biol Chem       Date:  2014-04-02       Impact factor: 5.157

2.  Laser synthesis: a solvent-free approach for the preparation of phenylthiazolo[5,4-b]pyridine derivatives.

Authors:  Rihab Jemili; Joana F Campos; Nicolas Dumuis; Hervé Rabat; Nadjib Semmar; Sabine Berteina-Raboin
Journal:  RSC Adv       Date:  2021-01-27       Impact factor: 3.361
  2 in total

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