开发基于天然蛋白酶体抑制剂衍生物的小分子药物共轭物，对表达 PSMA 的癌细胞具有选择性

IF 3.3 3区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic & Medicinal Chemistry Pub Date : 2024-06-03 DOI:10.1016/j.bmc.2024.117773

Takahiro Obara , Nanami Kawano , Kengo Tatsumi , Akira Katsuyama , Kohei Nakajima , Mikako Ogawa , Satoshi Ichikawa

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引用次数: 0

摘要

在这项研究中，我们开发了由前列腺特异性膜抗原（PSMA）配体和丁香油酚衍生物组成的小分子药物共轭物（SMDCs），后者是一种有效的蛋白酶体抑制剂，可选择性地将丁香油酚衍生物递送至前列腺癌细胞。两种母体化合物用于不同连接位点的丁香酚林衍生物。这些SMDCs具有PSMA表达细胞选择性细胞毒性，可用于更安全的癌症治疗。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Development of small molecule–drug conjugates based on derivatives of natural proteasome inhibitors that exhibit selectivity for PSMA-expressing cancer cells

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Development of small molecule–drug conjugates based on derivatives of natural proteasome inhibitors that exhibit selectivity for PSMA-expressing cancer cells

In this study, we have developed small molecule drug conjugates (SMDCs) consisting of a prostate specific membrane antigen (PSMA) ligand and syringolin derivatives, which are potent proteasome inhibitors, to selectively deliver syringolin derivatives to prostate cancer cells. Two parent compounds were used for syringolin derivatives with different linkage sites. These SMDCs exhibited PSMA-expressing cell-selective cytotoxicity and they could potentially be used for safer treatment of cancer.

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来源期刊

Bioorganic & Medicinal Chemistry 医学-生化与分子生物学

CiteScore

6.80

自引率

2.90%

发文量

413

审稿时长

17 days

期刊介绍： Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.