摘要
肽基精氨酸转亚胺基酶(PADs)是一类能使精氨酸残基在蛋白质的表面转换成瓜氨酸残基的同工酶。这通常是翻译后加工的一部分。PADs存在于大多数组织中,并且同工酶分布具有组织特异性。过去15年的研究表明,在包括神经系统疾病的某些疾病状态下,PADs上调或催化活性会增强。特别是,在神经退行性疾病如多发性硬化症,阿尔茨海默氏等病发生时,瓜氨酸含量和PAD活性增加。本文对PAD酶作为神经退行性疾病靶点进行了综述,并简要概述了从药物化学方面鉴定治疗各种神经退行性疾病的PAD抑制剂所做的工作。
关键词: 肽基精氨酸脱亚胺酶、神经退行性疾病,瓜氨酸化,翻译后修饰。
Current Medicinal Chemistry
Title:Peptidyl Arginine Deiminases and Neurodegenerative Diseases
Volume: 23 Issue: 2
Author(s): R. Tu, H.M. Grover and L.P. Kotra
Affiliation:
关键词: 肽基精氨酸脱亚胺酶、神经退行性疾病,瓜氨酸化,翻译后修饰。
摘要: Peptidyl arginine deiminases (PADs) are a small group of isozymes that convert Arg residues on the surface of proteins into citrulline residues, typically as a part of posttranslational processing. PADs are present in most of the tissues, and the isozyme distribution is tissue-specific. In the past 15 years, it is becoming apparent that PADs are either upregulated or their catalytic activity is enhanced in certain disease conditions, including neurological diseases. In particular, hypercitrullinated proteins and elevated PAD activities are discovered in neurodegenerative conditions such as multiple sclerosis, Alzheimer’s disease etc. This review article reviews the status of PAD enzymes as targets in neurodegenerative conditions, and briefly outlines the efforts in medicinal chemistry to identify PAD inhibitors for the treatment of various neurodegenerative conditions.
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Cite this article as:
R. Tu, H.M. Grover and L.P. Kotra , Peptidyl Arginine Deiminases and Neurodegenerative Diseases, Current Medicinal Chemistry 2016; 23 (2) . https://dx.doi.org/10.2174/0929867323666151118120710
DOI https://dx.doi.org/10.2174/0929867323666151118120710 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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