Hitting KRAS When It’s Down

Ronen Gabizon, Nir London

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)6677-6678
Number of pages2
JournalJournal of Medicinal Chemistry
Volume63
Issue number13
DOIs
StatePublished - 9 Jul 2020

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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