Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS<sup>G12C</sup> Inhibitor-Reference-Cited by-同舟云学术

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS^G12C Inhibitor

Published:2022-10-27 Issue:21 Volume:65 Page:14614-14629
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Bröker Joachim¹^ORCID,Waterson Alex G.²^ORCID,Smethurst Chris¹,Kessler Dirk¹^ORCID,Böttcher Jark¹,Mayer Moriz¹,Gmaschitz Gerhard¹,Phan Jason²,Little Andrew²,Abbott Jason R.²^ORCID,Sun Qi²,Gmachl Michael¹,Rudolph Dorothea¹,Arnhof Heribert¹,Rumpel Klaus¹,Savarese Fabio¹,Gerstberger Thomas¹,Mischerikow Nikolai¹,Treu Matthias¹,Herdeis Lorenz¹,Wunberg Tobias¹,Gollner Andreas¹^ORCID,Weinstabl Harald¹^ORCID,Mantoulidis Andreas¹,Krämer Oliver¹,McConnell Darryl B.¹^ORCID,W. Fesik Stephen²^ORCID

Affiliation:

1. Boehringer Ingelheim RCV GmbH & Co. KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria

2. Department of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States

Funder

National Cancer Institute

?sterreichische Forschungsf?rderungsgesellschaft

Lustgarten Foundation

National Institutes of Health

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c01120

Reference31 articles.