Sticking it to KRAS: Covalent Inhibitors Enter the Clinic
Open accessAbstract
Drugs that target KRAS 12C covalently, AMG 510 and MRTX849, are now in the clinic. Recent papers describe development of these compounds, their selectivity and properties, early clinical data, and potential combination therapies. These papers herald a new era in Ras research, with improved drugs and strategies certain to follow.
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- Authors
- McCormick, F.
- Affiliations
- University of California, San Francisco (US)
- Corresponding author
- McCormick, Frank
- ORCID
- McCormick, Frank
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2020-01
- Volume
- 37
- Issue
- 1
- Pages
- 3-4
- ISSN
- 1535-6108 (ISSN-L)
- PMC
- PMC7891852
- OpenAlex
- W2998764552
- Cited by
- 56
- References
- 10
- Citations by year
- 2026: 2 · 2025: 5 · 2024: 8 · 2023: 3 · 2022: 11 · 2021: 12 · 2020: 15
- FWCI
- 3.41
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Cancer Cell (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- eScholarship (California Digital Library) (submittedVersion)
- Funders
- National Cancer Institute (R35CA197709)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
- Keywords
- KRAS, covalent inhibitors, sotorasib, adagrasib, Ras signaling, drug development, drug selectivity, combination therapy, clinical trials
- MeSH terms
- Animals, Antineoplastic Agents, Drug Evaluation, Preclinical, Humans, Mutation, Neoplasms, Piperazines, Pyridines, Pyrimidines, Genes, ras, Drug Design, Signal Transduction, Proto-Oncogene Proteins p21(ras), Treatment Outcome, Mice, Translational Research, Biomedical
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