Drugging the Next Undruggable KRAS Allele-Gly12Asp

Qinheng Zheng; D Matthew Peacock; Kevan M Shokat

doi:10.1021/acs.jmedchem.2c00099

Drugging the Next Undruggable KRAS Allele-Gly12Asp

J Med Chem. 2022 Feb 24;65(4):3119-3122. doi: 10.1021/acs.jmedchem.2c00099. Epub 2022 Feb 15.

Authors

Qinheng Zheng¹, D Matthew Peacock¹, Kevan M Shokat¹

Affiliation

¹ Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California San Francisco, San Francisco, California 94158, United States.

PMID: 35167298
DOI: 10.1021/acs.jmedchem.2c00099

Abstract

Since its discovery as the first human oncogene in 1983, the small GTPase KRAS has been a major target of cancer drug discovery. The paper reported in this issue describes a long-awaited small molecule drug candidate of the oncogenic KRAS (G12D) mutant for the treatment of currently incurable pancreatic cancer.

Publication types

Review

MeSH terms

Alleles
Animals
Antineoplastic Agents / pharmacology*
Drug Discovery
Gene Expression Regulation, Neoplastic
Humans
Mutation
Pancreatic Neoplasms / drug therapy*
Pancreatic Neoplasms / genetics*
Proto-Oncogene Proteins p21(ras) / drug effects*
Proto-Oncogene Proteins p21(ras) / genetics*

Substances

Antineoplastic Agents
KRAS protein, human
Proto-Oncogene Proteins p21(ras)