拓展 TPD 视野：针对 BCL6 和 SMARCA2 的创新战略

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2024-04-26 DOI:10.1021/acsmedchemlett.4c00166

Robert B. Kargbo*,

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引用次数: 0

摘要

靶向蛋白降解（TPD）技术是癌症治疗领域的一种突破性方法，主要针对 BCL6 和 SMARCA2 等致癌蛋白的选择性降解。通过利用泛素-蛋白酶体系统，TPD 提供了一种超越传统疗法局限性的新策略，其目标是肿瘤发生的核心机制。本文探讨了 TPD 的重大进展，详细介绍了降解与癌症有牵连的重要蛋白质的创新策略，并讨论了这些方法通过精准医学和个性化疗法改变癌症治疗的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Expanding TPD Horizons: Innovative Strategies Targeting BCL6 and SMARCA2

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Expanding TPD Horizons: Innovative Strategies Targeting BCL6 and SMARCA2

Targeted protein degradation (TPD) technologies represent a groundbreaking approach in cancer therapy, focusing on the selective degradation of oncogenic proteins such as BCL6 and SMARCA2. By leveraging the ubiquitin-proteasome system, TPD offers a novel strategy that surpasses traditional therapies’ limitations, targeting the core mechanisms of oncogenesis. This article explores the significant advancements in TPD, detailing innovative strategies for the degradation of essential proteins implicated in cancer, and discusses the potential of these approaches to transform cancer treatment through precision medicine and personalized therapy.

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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.