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Article

NCP07: A potent ERα CBS-targeted degrader with dual-action against ESR1 mutations in breast cancer.

European journal of medicinal chemistry - 5 Nov 2026

Liang Jinsen, Wu Yihe, Yang Lanxin, Xu Bingjie, Wang Dandan, Shu Hong-Bing, Dong Chune, Li Shu, Zhou Hai-Bing

Abstract excerpt

ESR1 mutation-driven endocrine therapy (ET) resistance remains a major challenge in breast cancer therapy. Herein, by integrating the advantages of PROTAC technology and coactivator-binding site (CBS) targeting strategy in overcoming drug resistance, we developed a class of novel and potent ERα PROTAC degraders against ET-resistant breast cancer. Among them, compound NCP07 could potently degrade ERα and inhibited...

Read the complete abstract on PubMed

Topics

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Share to Antineoplastic Agents
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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Dose-Response Relationship, Drug

Share to Drug Resistance, Neoplasm

Share to Drug Screening Assays, Antitumor

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Source

Identifiers

PMID: 42391931
DOI: 10.1016/j.ejmech.2026.119113

Genes

CBS
ESR1
VHL

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

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