High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRAS<sup>G12C</sup> by Intact Protein MS and Targeted MRM-Reference-Cited by-同舟云学术

High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRAS^G12C by Intact Protein MS and Targeted MRM

Published:2022-01-06 Issue:2 Volume:94 Page:1230-1239
ISSN:0003-2700
Container-title:Analytical Chemistry
language:en
Short-container-title:Anal. Chem.

Author:

Li Ke Sherry¹^ORCID,Quinn John G.¹^ORCID,Saabye Matthew J.²,Guerrero Jesus F. Salcido¹,Nonomiya Jim¹,Lian Qihui³,Phung Wilson⁴,Izrayelit Yevgeniy¹,Walters Benjamin T.¹,Gustafson Amy¹,Endres Nicholas F.¹,Beresini Maureen H.¹,Mulvihill Melinda M.¹

Affiliation:

1. Biochemical and Cellular Pharmacology, Genentech, Inc., South San Francisco, California 94080, United States

2. Confluence, 4340 Duncan Avenue, Suite 400, St. Louis, Missouri 63110, United States

3. WuXi AppTec Co. Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China

4. Microchemistry, Proteomics and Lipidomics, Genentech Inc., South San Francisco, California 94080, United States

Funder

We thank John Tran and Margaret Porter Scott for reviewing the manuscript.

Publisher

American Chemical Society (ACS)

Subject

Analytical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.analchem.1c04463

Reference30 articles.

1. 10 years into the resurgence of covalent drugs

2. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

3. The resurgence of covalent drugs

4. The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

5. Drug discovery considerations in the development of covalent inhibitors

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