Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants.


Journal

Cancer discovery
ISSN: 2159-8290
Titre abrégé: Cancer Discov
Pays: United States
ID NLM: 101561693

Informations de publication

Date de publication:
01 04 2022
Historique:
received: 05 10 2021
revised: 12 11 2021
accepted: 03 12 2021
pubmed: 21 1 2022
medline: 6 4 2022
entrez: 20 1 2022
Statut: ppublish

Résumé

KRAS is the most frequently mutated oncogene, harboring mutations in approximately one in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment paradigm for patients with KRASG12C-mutated non-small cell lung cancer and colorectal cancer. The success of addressing a previously elusive KRAS allele has fueled drug discovery efforts for all KRAS mutants. Pan-KRAS drugs have the potential to address broad patient populations, including KRASG12D-, KRASG12V-, KRASG13D-, KRASG12R-, and KRASG12A-mutant or KRAS wild-type-amplified cancers, as well as cancers with acquired resistance to KRASG12C inhibitors. Here, we review actively pursued allele-specific and pan-KRAS inhibition strategies and their potential utility. Mutant-selective KRASG12C inhibitors target a fraction (approximately 13.6%) of all KRAS-driven cancers. A broad arsenal of KRAS drugs is needed to comprehensively conquer KRAS-driven cancers. Conceptually, we foresee two future classes of KRAS medicines: mutant-selective KRAS drugs targeting individual variant alleles and pan-KRAS therapeutics targeting a broad range of KRAS alterations.

Identifiants

pubmed: 35046095
pii: 2159-8290.CD-21-1331
doi: 10.1158/2159-8290.CD-21-1331
pmc: PMC9394389
mid: NIHMS1763757
doi:

Substances chimiques

KRAS protein, human 0
Proto-Oncogene Proteins p21(ras) EC 3.6.5.2

Types de publication

Journal Article Review Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

924-937

Subventions

Organisme : NCI NIH HHS
ID : P30 CA008748
Pays : United States

Informations de copyright

©2022 The Authors; Published by the American Association for Cancer Research.

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Auteurs

Marco H Hofmann (MH)

Discovery Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.

Daniel Gerlach (D)

Discovery Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.

Sandra Misale (S)

Molecular Pharmacology Program, Memorial Sloan-Kettering Cancer Center, New York, New York.

Mark Petronczki (M)

Discovery Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.

Norbert Kraut (N)

Discovery Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.

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Classifications MeSH