Targeting Oncogenic Pathways: Advances in KRAS, CDK, EGFR, and PROTAC-Based Therapies

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-03-11 DOI:10.1021/acsmedchemlett.5c0011110.1021/acsmedchemlett.5c00111

Robert B. Kargbo*,

引用次数: 0

Abstract

Recent advancements in cancer therapy focus on targeting critical mutations and regulatory pathways, particularly KRAS mutations and cyclin-dependent kinases (CDKs), which drive cancer progression. This Patent Highlight showcases the development of novel small-molecule inhibitors for KRAS and CDKs, highlighting their mechanisms of action, critical findings from preclinical studies, and the potential for improving therapeutic outcomes in cancers such as nonsmall cell lung cancer (NSCLC), colorectal, and pancreatic cancers.

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靶向致癌途径：KRAS， CDK， EGFR和基于protac的治疗进展

癌症治疗的最新进展集中在靶向关键突变和调控途径，特别是驱动癌症进展的KRAS突变和细胞周期蛋白依赖性激酶（CDKs）。该专利重点展示了KRAS和CDKs的新型小分子抑制剂的开发，强调了它们的作用机制，临床前研究的关键发现，以及改善非小细胞肺癌（NSCLC）、结直肠癌和胰腺癌等癌症治疗结果的潜力。

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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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.