Literature DB >> 18667312

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.

Wooyoung Hur1, Anastasia Velentza, Sungjoon Kim, Laura Flatauer, Xinnong Jiang, David Valente, Daniel E Mason, Melissa Suzuki, Brad Larson, Jianming Zhang, Anna Zagorska, Michael Didonato, Advait Nagle, Markus Warmuth, Steven P Balk, Eric C Peters, Nathanael S Gray.   

Abstract

Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ten other protein kinases including all five Tec-family members. We demonstrate that the Tec-family kinase Bmx is potently inhibited by irreversible modification at Cys496 by clinical stage EGFR inhibitors such as CI-1033. This cross-reactivity may have significant clinical implications.

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Year:  2008        PMID： 18667312      PMCID： PMC2610413          DOI： 10.1016/j.bmcl.2008.07.062

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


  13 in total

1.  Multicenter, randomized phase II trial of oral CI-1033 for previously treated advanced ovarian cancer.

Authors:  Susana Campos; Oday Hamid; Michael V Seiden; Amit Oza; Marie Plante; Ronald K Potkul; Peter F Lenehan; Eric P Kaldjian; Mary L Varterasian; Cheryl Jordan; Claudie Charbonneau; Hal Hirte
Journal:  J Clin Oncol       Date:  2005-08-20       Impact factor: 44.544

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.  2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.

Authors:  Allan Wissner; M Brawner Floyd; Bernard D Johnson; Heidi Fraser; Charles Ingalls; Thomas Nittoli; Russell G Dushin; Carolyn Discafani; Ramaswamy Nilakantan; Joseph Marini; Malini Ravi; Kinwang Cheung; Xingzhi Tan; Sylvia Musto; Tami Annable; Marshall M Siegel; Frank Loganzo
Journal:  J Med Chem       Date:  2005-12-01       Impact factor: 7.446

4.  Etk/Bmx as a tumor necrosis factor receptor type 2-specific kinase: role in endothelial cell migration and angiogenesis.

Authors:  Shi Pan; Ping An; Rong Zhang; Xiangrong He; Guoyong Yin; Wang Min
Journal:  Mol Cell Biol       Date:  2002-11       Impact factor: 4.272

5.  Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.

Authors:  Eunice L Kwak; Raffaella Sordella; Daphne W Bell; Nadia Godin-Heymann; Ross A Okimoto; Brian W Brannigan; Patricia L Harris; David R Driscoll; Panos Fidias; Thomas J Lynch; Sridhar K Rabindran; John P McGinnis; Allan Wissner; Sreenath V Sharma; Kurt J Isselbacher; Jeffrey Settleman; Daniel A Haber
Journal:  Proc Natl Acad Sci U S A       Date:  2005-05-16       Impact factor: 11.205

6.  Structural bioinformatics-based design of selective, irreversible kinase inhibitors.

Authors:  Michael S Cohen; Chao Zhang; Kevan M Shokat; Jack Taunton
Journal:  Science       Date:  2005-05-27       Impact factor: 47.728

7.  Etk/Bmx, a tyrosine kinase with a pleckstrin-homology domain, is an effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells.

Authors:  Y Qiu; D Robinson; T G Pretlow; H J Kung
Journal:  Proc Natl Acad Sci U S A       Date:  1998-03-31       Impact factor: 11.205

8.  Activation of nonreceptor tyrosine kinase Bmx/Etk mediated by phosphoinositide 3-kinase, epidermal growth factor receptor, and ErbB3 in prostate cancer cells.

Authors:  Xinnong Jiang; Robert A Borgesi; Nicole C McKnight; Ramneet Kaur; Christopher L Carpenter; Steven P Balk
Journal:  J Biol Chem       Date:  2007-09-06       Impact factor: 5.157

9.  Antisense oligodeoxynucleotides to the blk tyrosine kinase prevent anti-mu-chain-mediated growth inhibition and apoptosis in a B-cell lymphoma.

Authors:  X R Yao; D W Scott
Journal:  Proc Natl Acad Sci U S A       Date:  1993-09-01       Impact factor: 11.205

10.  Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.

Authors:  D W Fry; A J Bridges; W A Denny; A Doherty; K D Greis; J L Hicks; K E Hook; P R Keller; W R Leopold; J A Loo; D J McNamara; J M Nelson; V Sherwood; J B Smaill; S Trumpp-Kallmeyer; E M Dobrusin
Journal:  Proc Natl Acad Sci U S A       Date:  1998-09-29       Impact factor: 11.205
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  14 in total

1.  A structure-guided approach to creating covalent FGFR inhibitors.

Authors:  Wenjun Zhou; Wooyoung Hur; Ultan McDermott; Amit Dutt; Wa Xian; Scott B Ficarro; Jianming Zhang; Sreenath V Sharma; Joan Brugge; Matthew Meyerson; Jeffrey Settleman; Nathanael S Gray
Journal:  Chem Biol       Date:  2010-03-26

2.  A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkC481S mutation in B-cell malignancies.

Authors:  Fu Gui; Jie Jiang; Zhixiang He; Li Li; Yunzhan Li; Zhou Deng; Yue Lu; Xinrui Wu; Guyue Chen; Jingyi Su; Siyang Song; Yue-Ming Zhang; Cai-Hong Yun; Xin Huang; Ellen Weisberg; Jianming Zhang; Xianming Deng
Journal:  Br J Pharmacol       Date:  2019-12-09       Impact factor: 8.739

Review 3.  Developing irreversible inhibitors of the protein kinase cysteinome.

Authors:  Qingsong Liu; Yogesh Sabnis; Zheng Zhao; Tinghu Zhang; Sara J Buhrlage; Lyn H Jones; Nathanael S Gray
Journal:  Chem Biol       Date:  2013-02-21

4.  Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.

Authors:  Yanke Liang; Melissanne de Wispelaere; Margot Carocci; Qingsong Liu; Jinhua Wang; Priscilla L Yang; Nathanael S Gray
Journal:  ACS Med Chem Lett       Date:  2017-02-03       Impact factor: 4.345

5.  Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.

Authors:  Eric R Goedken; Maria A Argiriadi; David L Banach; Bryan A Fiamengo; Sage E Foley; Kristine E Frank; Jonathan S George; Christopher M Harris; Adrian D Hobson; David C Ihle; Douglas Marcotte; Philip J Merta; Mark E Michalak; Sara E Murdock; Medha J Tomlinson; Jeffrey W Voss
Journal:  J Biol Chem       Date:  2014-12-31       Impact factor: 5.157

6.  Ibrutinib (ImbruvicaTM) potently inhibits ErbB receptor phosphorylation and cell viability of ErbB2-positive breast cancer cells.

Authors:  Nicole Grabinski; Florian Ewald
Journal:  Invest New Drugs       Date:  2014-08-01       Impact factor: 3.850

7.  RAF1-MEK1-ERK/AKT axis may confer NSCLC cell lines resistance to erlotinib.

Authors:  Zhi-Hong Xu; Jun-Biao Hang; Jia-An Hu; Bei-Li Gao
Journal:  Int J Clin Exp Pathol       Date:  2013-07-15

8.  Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Authors:  Wenjun Zhou; Dalia Ercan; Liang Chen; Cai-Hong Yun; Danan Li; Marzia Capelletti; Alexis B Cortot; Lucian Chirieac; Roxana E Iacob; Robert Padera; John R Engen; Kwok-Kin Wong; Michael J Eck; Nathanael S Gray; Pasi A Jänne
Journal:  Nature       Date:  2009-12-24       Impact factor: 49.962

9.  Endothelial Bmx tyrosine kinase activity is essential for myocardial hypertrophy and remodeling.

Authors:  Tanja Holopainen; Markus Räsänen; Andrey Anisimov; Tomi Tuomainen; Wei Zheng; Denis Tvorogov; Juha J Hulmi; Leif C Andersson; Bruno Cenni; Pasi Tavi; Eero Mervaala; Riikka Kivelä; Kari Alitalo
Journal:  Proc Natl Acad Sci U S A       Date:  2015-10-01       Impact factor: 11.205

10.  BMX Negatively Regulates BAK Function, Thereby Increasing Apoptotic Resistance to Chemotherapeutic Drugs.

Authors:  Joanna L Fox; Alan Storey
Journal:  Cancer Res       Date:  2015-02-03       Impact factor: 12.701
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