A Noncovalent KRASG12D Inhibitor Shows Potent and Selective Activity
Abstract
MRTX1133 is a high-affinity, selective, and potent KRASG12D inhibitor with antitumor efficacy.
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MRTX-1133 inhibited KRAS-dependent signaling and promoted tumor regression in xenograft models.
“Besides, MRTX-1133 inhibited KRAS-dependent signaling and promoted tumor regression in xenograft models.”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [256]
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Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · see citing works
- Venue
- Cancer Discovery
- Published
- 2022-10-21
- Volume
- 12
- Issue
- 12
- Pages
- OF8-OF8
- ISSN
- 2159-8274 (ISSN-L)
- 2159-8290
- OpenAlex
- W4307034052
- Cited by
- 2
- References
- 0
- Citations by year
- 2024: 1 · 2023: 1
- FWCI
- 0.16
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Cancer Discovery (publishedVersion)
- PubMed (publishedVersion)
- 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 G12D, MRTX1133, KRAS inhibitors, non-covalent inhibitors, small molecule inhibitors, antitumor efficacy, oncogenic KRAS, drug selectivity
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