β-Glucuronidase-Responsive Albumin-Binding Prodrug of Colchicine-Site Binders for Selective cancer Therapy.

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2025-01-21 DOI:10.1002/cmdc.202400969

Alexandra Bordes, Isabelle Opalinski, Fabien Thoreau, Olivier Provot, Mouad Alami, Abdallah Hamze, Sébastien Papot

引用次数: 0

Abstract

The development of novel therapeutic strategies enabling the selective destruction of tumors while sparing healthy tissues is of great interest to improve the efficacy of cancer chemotherapy. In this context, we designed a β-glucuronidase-responsive albumin-binding prodrug programmed to release a potent Isocombretastatin A-4 analog within the tumor microenvironment. When injected at a non-toxic dose in mice bearing orthotopic triple-negative mammary tumors, this prodrug produced a significant anticancer activity, therefore offering a valuable alternative to the systemic administration of the parent drug.

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β-葡萄糖醛酸酶反应性白蛋白结合前药的秋水仙碱位点结合剂选择性癌症治疗。

在保留健康组织的情况下选择性破坏肿瘤的新治疗策略的发展对提高癌症化疗的疗效具有重要意义。在这种情况下，我们设计了一种β-葡萄糖醛酸酶反应性白蛋白结合前药，该前药被编程为在肿瘤微环境中释放一种有效的Isocombretastatin a -4类似物。当以无毒剂量注射到患有原位三阴性乳腺肿瘤的小鼠时，该前药产生了显著的抗癌活性，因此为母体药物的全身给药提供了有价值的替代方案。

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

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

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