人碳酸酐酶抑制剂

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-09-03 DOI:10.1021/acsmedchemlett.5c00443

Claudiu T. Supuran*,

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引用次数: 0

摘要

人类编码金属酶碳酸酐酶（CA, EC 4.2.1.1）的15种异构体，它催化二氧化碳和碳酸氢盐之间的相互转化，并参与许多生理/病理过程。CA抑制剂在临床上用作利尿剂、抗青光眼药、抗癫痫药和抗肥胖药。作为抗肿瘤/抗转移药物，或用于脑缺血，类风湿关节炎和神经退行性疾病的管理的新应用，讨论了超过45种具有抑制这些酶特性的化学型。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Human Carbonic Anhydrase Inhibitors

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Human Carbonic Anhydrase Inhibitors

Humans encode 15 isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), which catalyzes the interconversion between CO₂ and bicarbonate and is involved in a multitude of physiological/pathological processes. CA inhibitors are in clinical use as diuretics, anti-glaucoma drugs, anti-epileptics, and anti-obesity agents. Novel applications as anti-tumor/anti-metastatic agents, or for the management of cerebral ischemia, rheumatoid arthritis, and neurodegenerative conditions, are discussed for the more than 45 chemotypes with inhibitory properties against these enzymes.

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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.