KRAS-G12C in the crosshairs

被引：25

作者：

Seton-Rogers, Sarah

机构：

[1] Nature Reviews Cancer,

来源：

NATURE REVIEWS CANCER | 2020年 / 20卷 / 01期

关键词：

D O I：

10.1038/s41568-019-0228-3

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Two papers report the discovery and preclinical analyses of two different covalent inhibitors of KRAS-G12C (AMG 510 and MRTX849) as well as the first data on the efficacy of these inhibitors in cancer patients.

引用

页码：3 / 3

页数：1

共 4 条

[1] The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity [J].

Canon, Jude ;

Rex, Karen ;

Saiki, Anne Y. ;

Mohr, Christopher ;

Cooke, Keegan ;

Bagal, Dhanashri ;

Gaida, Kevin ;

Holt, Tyler ;

Knutson, Charles G. ;

Koppada, Neelima ;

Lanman, Brian A. ;

Werner, Jonathan ;

Rapaport, Aaron S. ;

San Miguel, Tisha ;

Ortiz, Roberto ;

Osgood, Tao ;

Sun, Ji-Rong ;

Zhu, Xiaochun ;

McCarter, John D. ;

Volak, Laurie P. ;

Houk, Brett E. ;

Fakih, Marwan G. ;

O'Neil, Bert H. ;

Price, Timothy J. ;

Falchook, Gerald S. ;

Desai, Jayesh ;

Kuo, James ;

Govindan, Ramaswamy ;

Hong, David S. ;

Ouyang, Wenjun ;

Henary, Haby ;

Arvedson, Tara ;

Cee, Victor J. ;

Lipford, J. Russell .

NATURE, 2019, 575 (7781) :217-+

[2] The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients [J].

Hallin, Jill ;

Engstrom, Lars D. ;

Hargis, Lauren ;

Calinisan, Andrew ;

Aranda, Ruth ;

Briere, David M. ;

Sudhakar, Niranjan ;

Bowcut, Vickie ;

Baer, Brian R. ;

Ballard, Joshua A. ;

Burkard, Michael R. ;

Fell, Jay B. ;

Fischer, John P. ;

Vigers, Guy P. ;

Xue, Yaohua ;

Gatto, Sole ;

Fernandez-Banet, Julio ;

Pavlicek, Adam ;

Velastagui, Karen ;

Chao, Richard C. ;

Barton, Jeremy ;

Pierobon, Mariaelena ;

Baldelli, Elisa ;

Patricoin, Emanuel F., III ;

Cassidy, Douglas P. ;

Marx, Matthew A. ;

Rybkin, Igor I. ;

Johnson, Melissa L. ;

Ou, Sai-Hong Ignatius ;

Lito, Piro ;

Papadopoulos, Kyriakos P. ;

Janne, Pasi A. ;

Olson, Peter ;

Christensen, James G. .

CANCER DISCOVERY, 2020, 10 (01) :54-71

[3] A model for RAS mutation patterns in cancers: finding the sweet spot [J].

Li, Siqi ;

Balmain, Allan ;

Counter, Christopher M. .

NATURE REVIEWS CANCER, 2018, 18 (12) :767-777

[4] K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions [J].

Ostrem, Jonathan M. ;

Peters, Ulf ;

Sos, Martin L. ;

Wells, James A. ;

Shokat, Kevan M. .

NATURE, 2013, 503 (7477) :548-+

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