Discovery of Highly Efficacious CRBN-Based KRAS Degraders Targeting Cancers with KRAS G12D and G12V Mutations.

doi:10.1021/acs.jmedchem.6c01153

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Article

Discovery of Highly Efficacious CRBN-Based KRAS Degraders Targeting Cancers with KRAS G12D and G12V Mutations.

Journal of medicinal chemistry - 10 Sept 2026

Wang Changwei, Ghosh Prithwish, Jin Shicheng, Bai Longchuan, Aguilar Angelo, McEachern Donna, Wang Mi, Li Qiuxia, Wen Bo, Sun Duxin, Wang Shaomeng

Abstract excerpt

KRAS G12D and G12V mutants account for >50% of human cancers carrying a mutated KRAS protein, and targeting KRAS proteins by induced protein degradation represents an attractive cancer therapeutic strategy. Herein, we present the design, synthesis, and evaluation of PROTAC KRAS degraders using a novel cereblon ligand, which led to the discovery of CW-10201 as a promising KRAS degrader. CW-10201 effectively...

Read the complete abstract on PubMed

Topics

Humans
Animals
Proto-Oncogene Proteins p21(ras)
Mice
Mutation
Antineoplastic Agents

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Cell Line, Tumor

Proteolysis Targeting Chimera

Ubiquitin-Protein Ligases

Adaptor Proteins, Signal Transducing

Structure-Activity Relationship

Cell Proliferation

Xenograft Model Antitumor Assays

Drug Discovery

Female

Proteolysis

Source

Open in PubMed Open full text

Identifiers

PMID: 42720481
DOI: 10.1021/acs.jmedchem.6c01153
PMCID: PMC13576394

Genes

KRAS
CRBN

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 23 Oct 2026.

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