Innovative Therapeutic Approaches Targeting K-Ras: Analysis of Macrocyclic Compounds, Peptidomimetics, and Pyridopyrimidine Inhibitors

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL ACS Medicinal Chemistry Letters Pub Date : 2024-07-25 DOI:10.1021/acsmedchemlett.4c00328

Robert B. Kargbo

引用次数: 0

Abstract

This Patent Highlight presents a detailed analysis of three novel classes of compounds designed to inhibit multiple forms of the K-Ras protein, as described in three patent applications. These patents cover macrocyclic compounds, peptidomimetics, and pyridopyrimidine inhibitors. This work explores each invention’s design, mechanism of action, relevance to cancer treatment, and results from assays demonstrating the efficacy of these compounds. The findings highlight the significant potential of these compounds in inhibiting tumor growth and inducing apoptosis in cancer cells, offering promising therapeutic options for K-Ras-driven cancers.

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针对 K-Ras 的创新治疗方法：分析大环化合物、拟肽化合物和吡啶嘧啶抑制剂

本专利摘要详细分析了三项专利申请中描述的三类新型化合物，这些化合物旨在抑制多种形式的 K-Ras 蛋白。这些专利涉及大环化合物、拟肽化合物和吡啶嘧啶抑制剂。这项研究探讨了每项发明的设计、作用机制、与癌症治疗的相关性，以及证明这些化合物疗效的实验结果。研究结果凸显了这些化合物在抑制肿瘤生长和诱导癌细胞凋亡方面的巨大潜力，为 K-Ras 驱动的癌症提供了前景广阔的治疗方案。

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.

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