利用新型双功能降解剂靶向降解BCL6: BCL6阳性癌症的新治疗策略

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-04-09 DOI:10.1021/acsmedchemlett.5c0018110.1021/acsmedchemlett.5c00181

Robert B. Kargbo*,

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引用次数: 0

摘要

BCL6过表达驱动b细胞恶性肿瘤的淋巴瘤发生和免疫逃避。本专利重点展示了针对BCL6的新型双功能降解物，具有高效力和选择性。这些降解物通过基于protac的机制诱导BCL6降解，导致BCL6阳性癌症的细胞凋亡和肿瘤消退。这种有针对性的方法提高了疗效和治疗潜力。

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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Targeted Degradation of BCL6 Using Novel Bifunctional Degraders: A New Therapeutic Strategy for BCL6-Positive Cancers

BCL6 overexpression drives lymphomagenesis and immune evasion in B-cell malignancies. This Patent Highlight presents novel bifunctional degraders targeting BCL6, demonstrating high potency and selectivity. These degraders induce BCL6 degradation via a PROTAC-based mechanism, resulting in apoptosis and tumor regression in BCL6-positive cancers. This targeted approach offers enhanced efficacy and therapeutic potential.

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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.