超越第一代KRAS抑制剂：BBO-8520验证双重机制假说。

IF 29.7 1区医学 Q1 ONCOLOGY

Cancer discovery Pub Date : 2025-03-03 DOI:10.1158/2159-8290.CD-24-1885

Zhiwei Zhou, Kenneth D Westover

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引用次数: 0

摘要

这一问题突出了一类小分子共价KRASG12C抑制剂boo -8520的开发，该抑制剂可同时靶向KRAS的活性（ON）和非活性（OFF）状态。这种双状态靶向为克服限制第一代KRAS抑制剂疗效的耐药机制提供了重要机会，并解决了KRAS靶向治疗的关键挑战。参见Maciag等人的相关文章，第578页。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Beyond First-Generation KRAS Inhibitors: BBO-8520 Tests the Dual Mechanism Hypothesis.

This issue highlights the development of a first-in-class small-molecule covalent KRASG12C inhibitor, BBO-8520, which targets both the active (ON) and inactive (OFF) states of KRAS. This dual-state targeting offers a significant opportunity to overcome the resistance mechanisms that have limited the efficacy of first-generation KRAS inhibitors and addresses critical challenges in KRAS-targeted therapy. See related article by Maciag et al., p. 578.

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来源期刊

Cancer discovery ONCOLOGY-

CiteScore

22.90

自引率

1.40%

发文量

838

审稿时长

6-12 weeks

期刊介绍： Cancer Discovery publishes high-impact, peer-reviewed articles detailing significant advances in both research and clinical trials. Serving as a premier cancer information resource, the journal also features Review Articles, Perspectives, Commentaries, News stories, and Research Watch summaries to keep readers abreast of the latest findings in the field. Covering a wide range of topics, from laboratory research to clinical trials and epidemiologic studies, Cancer Discovery spans the entire spectrum of cancer research and medicine.