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淋病奈瑟菌碳酸酐酶抑制作用。

Neisseria gonorrhoeae carbonic anhydrase inhibition.

机构信息

Borch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN, United States.

Borch Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN, United States.

出版信息

Enzymes. 2024;55:243-281. doi: 10.1016/bs.enz.2024.05.008. Epub 2024 Jun 6.

Abstract

Carbonic anhydrases (CAs) are ubiquitous enzymes that are found in all kingdoms of life. Though different classes of CAs vary in their roles and structures, their primary function is to catalyze the reaction between carbon dioxide and water to produce bicarbonate and a proton. Neisseria gonorrhoeae encodes for three distinct CAs (NgCAs) from three different families: an α-, a β-, and a γ-isoform. This chapter details the differences between the three NgCAs, summarizing their subcellular locations, roles, essentiality, structures, and enzyme kinetics. These bacterial enzymes have the potential to be drug targets; thus, previous studies have investigated the inhibition of NgCAs-primarily the α-isoform. Therefore, the classes of inhibitors that have been shown to bind to the NgCAs will be discussed as well. These classes include traditional CA inhibitors, such as sulfonamides, phenols, and coumarins, as well as non-traditional inhibitors including anions and thiocarbamates.

摘要

碳酸酐酶(CA)是普遍存在于所有生命领域的酶。尽管不同类别的 CA 在作用和结构上有所不同,但它们的主要功能是催化二氧化碳和水之间的反应,生成碳酸氢盐和质子。淋病奈瑟菌编码三种不同家族的三种独特的 CA(NgCAs):一种α-、一种β-和一种γ-同工酶。本章详细介绍了三种 NgCA 之间的差异,总结了它们的亚细胞定位、作用、必需性、结构和酶动力学。这些细菌酶具有成为药物靶点的潜力;因此,以前的研究已经调查了 NgCA 的抑制作用-主要是α-同工酶。因此,将讨论与 NgCA 结合的抑制剂类别。这些类别包括传统的 CA 抑制剂,如磺胺类、酚类和香豆素类,以及非传统的抑制剂,包括阴离子和硫代氨基甲酸盐。

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