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荧光和自旋标记的碳酸酐酶抑制剂。

Fluorescence- and spin-labeled carbonic anhydrase inhibitors.

作者信息

Cecchi Alessandro, Supuran Claudiu T

机构信息

Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.

出版信息

Curr Pharm Des. 2008;14(7):699-707. doi: 10.2174/138161208783877839.

Abstract

Carbonic anhydrase IX (hCA IX) is a membrane-associated glycoprotein that is observed in many tumor tissues and is strongly overexpressed by hypoxia conditions. Hypoxia is a clinically important tumor parameter and this enzyme can play an important role as a potential marker of hypoxic tumor and as a therapeutic target too. In the last years, Carbonic Anhydrase IX Inhibitors which possess fluorescent probe were largely used for visualize hypoxic tumor cell lines and for understanding the biological roles of hCA IX in acidification of the external matrix. Here we resume the development pathways of such compounds from the design to the final biological evaluation. Furthermore, spin-labeled CAIs were included to have a complete overview of the potentiality of this enzyme as marker of hypoxic tumors.

摘要

碳酸酐酶IX(hCA IX)是一种膜相关糖蛋白,在许多肿瘤组织中都有发现,并且在缺氧条件下会强烈过表达。缺氧是一个临床上重要的肿瘤参数,这种酶作为缺氧肿瘤的潜在标志物以及治疗靶点都可以发挥重要作用。在过去几年中,带有荧光探针的碳酸酐酶IX抑制剂被大量用于可视化缺氧肿瘤细胞系以及了解hCA IX在细胞外基质酸化中的生物学作用。在此,我们总结了此类化合物从设计到最终生物学评估的研发历程。此外,还纳入了自旋标记的CAIs,以便全面了解这种酶作为缺氧肿瘤标志物的潜力。

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