Affordable Access

deepdyve-link
Publisher Website

Hitting KRAS When It’s Down

Authors
  • Gabizon, Ronen
  • London, Nir
Type
Published Article
Journal
Journal of Medicinal Chemistry
Publisher
American Chemical Society
Publication Date
Jun 22, 2020
Volume
63
Issue
13
Pages
6677–6678
Identifiers
DOI: 10.1021/acs.jmedchem.0c00785
PMID: 32568546
PMCID: PMC7467708
Source
PubMed Central
License
Unknown

Abstract

KRAS, one of the most prevalent oncogenes and sought-after anticancer targets, has eluded chemists for decades until an irreversible covalent strategy targeting a specific mutation (G12C) paved the way for the first KRAS inhibitors to reach the clinic. MRTX849 is one such clinical candidate with promising initial results in patients harboring the mutation. The impressive optimization story of MRTX849 highlights challenges and solutions in the development of covalent drugs, including the use of an α-fluoroacrylamide electrophile.

Report this publication

Statistics

Seen <100 times