Targeted Treatment of Cancer by Using Conjugate Compounds with Poly(ADP-ribose) Polymerase (PARP) Inhibitors.

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-06-18 eCollection Date: 2025-07-10 DOI:10.1021/acsmedchemlett.5c00341

Xin Zhou, Steven H Liang

引用次数: 0

Abstract

This patent describes a novel therapeutic strategy involving conjugate compounds that integrate a poly-(ADP-ribose) polymerase (PARP) inhibitor moiety with a disease-targeting ligand, offering a dual-function approach for the treatment of cancer. These conjugates are designed to enhance the efficacy of targeted radionuclide therapies by selectively delivering PARP inhibition to tumor cells, thereby disrupting DNA repair mechanisms and increasing cancer cell susceptibility to DNA damage-induced cytotoxicity.

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聚（adp -核糖）聚合酶（PARP）抑制剂缀合物靶向治疗癌症

该专利描述了一种新的治疗策略，涉及将多（adp -核糖）聚合酶（PARP）抑制剂片段与疾病靶向配体结合的共轭化合物，为癌症治疗提供了双重功能方法。这些偶联物旨在通过选择性地将PARP抑制作用传递给肿瘤细胞，从而破坏DNA修复机制，增加癌细胞对DNA损伤诱导的细胞毒性的易感性，从而提高靶向放射性核素治疗的疗效。

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.