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碳酸酐酶抑制剂作为治疗肥胖症的新兴药物。

Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity.

出版信息

Expert Opin Emerg Drugs. 2012 Mar;17(1):11-5. doi: 10.1517/14728214.2012.664132. Epub 2012 Feb 16.

DOI:10.1517/14728214.2012.664132
PMID:22335448
Abstract

Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes in mammals, being involved in numerous biosynthetic processes, including gluconeogenesis, lipogenesis and ureagenesis. It has recently emerged that CA inhibitors (CAIs) targeting the mitochondrial isoforms CA VA and VB have potential as novel antiobesity drugs. This Editorial discusses the biochemical and biological rationale for the use of CAIs in the management of obesity.

摘要

碳酸酐酶(CAs,EC 4.2.1.1)是哺乳动物中普遍存在的金属酶,参与许多生物合成过程,包括糖异生、脂肪生成和尿素生成。最近发现,针对线粒体同工型 CA VA 和 VB 的 CA 抑制剂(CAI)有作为新型减肥药的潜力。本社论讨论了在肥胖症管理中使用 CAI 的生化和生物学依据。

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Carbonic anhydrase inhibitors. Identification of selective inhibitors of the human mitochondrial isozymes VA and VB over the cytosolic isozymes I and II from a natural product-based phenolic library.碳酸酐酶抑制剂。从基于天然产物的酚类文库中鉴定出对人线粒体同工酶 VA 和 VB 具有选择性抑制作用的抑制剂,而对胞质同工酶 I 和 II 则没有抑制作用。
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