选择性PARP1抑制剂治疗癌症的研究进展

IF 3.9 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2026-07-09 Epub Date: 2026-06-23 DOI:10.1021/acsmedchemlett.6c00296

Xin Zhou, and , Steven H. Liang*,

引用次数: 0

摘要

PARP1是一种关键的DNA损伤反应酶，通过parp介导的DNA修复支持肿瘤细胞存活。尽管fda批准的PARP抑制剂已经验证了这种治疗策略，但有限的PARP1/PARP2选择性可能会导致不良反应。本专利公开了具有改进效力、选择性和脑渗透药代动力学特性的下一代PARP1抑制剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

Development of Selective PARP1 Inhibitors for the Treatment of Cancer

PARP1 is a key DNA damage response enzyme that supports tumor-cell survival through PARP-mediated DNA repair. Although FDA-approved PARP inhibitors have validated this therapeutic strategy, limited PARP1/PARP2 selectivity may cause adverse effects. This patent discloses next-generation PARP1 inhibitors with improved potency, selectivity, and brain-penetrant pharmacokinetic properties.

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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.