靶向KRAS G12D和G10突变的新型小分子抑制剂

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-05-16 eCollection Date: 2025-06-12 DOI:10.1021/acsmedchemlett.5c00264

Robert B Kargbo

引用次数: 0

摘要

KRAS突变，特别是G12D和G10，在多种癌症中驱动肿瘤发生。最近的专利WO 2025/054347 A1和WO 2025/054530 A1披露了选择性靶向这些突变的新型小分子抑制剂，显示出高效，良好的药代动力学，并在胰腺癌，肺癌和结直肠癌中具有良好的治疗潜力。

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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Targeting KRAS G12D and G10 Mutations with Novel Small Molecule Inhibitors.

KRAS mutations, particularly G12D and G10, drive oncogenesis in multiple cancers. Recent patents WO 2025/054347 A1 and WO 2025/054530 A1 disclose novel small molecule inhibitors that selectively target these mutations, demonstrating high potency, favorable pharmacokinetics, and promising therapeutic potential in challenging pancreatic, lung, and colorectal cancers.

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来源期刊

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.