以组氨酸为靶点开发新一代共价酶抑制剂

Q4 Pharmacology, Toxicology and Pharmaceutics
D. Poirier
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引用次数: 1

摘要

尽管多年来开发了大量的不可逆抑制剂,但对这种类型的治疗分子仍然存在强烈的偏见,特别是在药物开发领域。然而,新一代的共价靶向抑制剂正在开发中,人们的兴趣也越来越大。事实上,新一代共价抑制剂具有弱活性物质(战斗部),能够在特定环境下选择性地与给定的氨基酸残基形成化学键,这种化学键可以是不可逆的,也可以是可逆的。除了新的选择性弹头,新的氨基酸也是目标。在下面的文章中,我们将重点关注共价靶向抑制剂选择性烷基化组氨酸。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Targeting histidine for developing a new generation of covalent enzyme inhibitors
Despite the significant number of irreversible inhibitors developed over the years, strong prejudices remain for this type of therapeutic molecule, particularly in the area of drug development. New generations of covalent targeted inhibitors are, however, in development, and interest is increasingly growing. In fact, the new generation of covalent inhibitors has a weakly reactive species (warhead) that is able, in a particular context, to selectively form a chemical bond with a given amino acid residue, which can be irreversible or reversible. In addition to new selective warheads, new amino acids are also targeted. In the following text, we will focus on covalent targeted inhibitors that selectively alkylate histidine.
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来源期刊
Current Enzyme Inhibition
Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
1.30
自引率
0.00%
发文量
30
期刊介绍: Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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