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Article

Discovery of a Potent and Selective KRAS G12D Degrader based on PROTAC Degradation.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences - 1 Nov 2026

Jiang Lili, Yang Wenyan, Liu Yanqing, Li Gangjian, Luo Xiaomin, Zhou Yubo, Qin Jiangjiang, Pan Youlu, Huang Wenhai

Abstract excerpt

KRAS-G12D has long been regarded as an intractable therapeutic target due to the flat binding pocket and its strong affinity for GTP/GDP. Proteolysis-targeting chimera (PROTAC) is a revolutionary drug discovery strategy that, by virtue of its unique pharmacological mode of action, provides more options for targeting undruggable targets. In this study, we designed and synthesized 20 novel KRAS G12D PROTACs based...

Read the complete abstract on PubMed

Topics

Proteolysis Targeting Chimera
Humans
Proto-Oncogene Proteins p21(ras)
Structure-Activity Relationship
Proteolysis

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

Cell Line, Tumor

Mutation

Antineoplastic Agents

Drug Discovery

Source

Identifiers

PMID: 42603637
DOI: 10.1016/j.ejps.2026.107633

Genes

KRAS

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 25 Oct 2026.

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