A New Frontier in Targeted Therapies: Harnessing PROTACs and Advanced Delivery Systems

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2024-10-15 DOI:10.1021/acsmedchemlett.4c0048910.1021/acsmedchemlett.4c00489

Robert B. Kargbo*,

引用次数: 0

Abstract

In the rapidly evolving field of oncology, the need for innovative therapeutic strategies is more pressing than ever. Many cancers, especially those driven by gene mutations like KRAS, remain challenging to treat. Traditional approaches, which often rely on small-molecule inhibitors, face significant limitations, particularly in addressing “undruggable” targets or delivering large therapeutic molecules across cellular membranes. As highlighted by four essential patents, the recent advancements in Proteolysis Targeting Chimeras (PROTACs) and intracellular delivery systems offer novel and promising strategies to overcome these challenges.

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靶向治疗的新领域：利用 PROTAC 和先进给药系统

在快速发展的肿瘤学领域，对创新治疗策略的需求比以往任何时候都更加迫切。许多癌症，尤其是那些由 KRAS 等基因突变驱动的癌症，仍然难以治疗。传统方法通常依赖于小分子抑制剂，但面临着很大的局限性，尤其是在解决 "不可药用 "靶点或跨细胞膜递送大分子治疗药物方面。正如四项重要专利所强调的，蛋白质分解靶向嵌合体（PROTACs）和细胞内递送系统的最新进展为克服这些挑战提供了新颖而有前景的策略。

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.