期刊
JOURNAL OF PHARMACEUTICAL ANALYSIS
卷 11, 期 1, 页码 15-27出版社
ELSEVIER
DOI: 10.1016/j.jpha.2020.03.012
关键词
Catechol-O-Methyltransferase (COMT); Enzymatic activity; Probe substrate; COMT inhibitor; High-throughput screening
资金
- National Key Research and Development Program of China [2017YFC1700200, 2017YFC1702000]
- National Natural Science Foundation of China [81922070, 81703604, 81973286, 81773687, 81603187]
- Natural Science Foundation of Shanghai [18ZR1436500]
- Program of Shanghai Academic/Technology Research Leader [18XD1403600]
- Shuguang Program by Shanghai Education Development Foundation [18SG40]
- Shanghai Municipal Education Commission
- development fund for Shanghai talents (2019)
- Key Science and Technology Program of Shenyang by Shenyang Science and Technology Bureau [17-230-9-05]
This review summarizes recent advances in analytical methodologies for sensing COMT activity and their applications, while highlighting challenges and future perspectives in the field. The practical assays for measuring COMT activities in complex biological samples are crucial for investigating the relevance of COMT to human diseases and promoting the discovery of COMT inhibitors via high-throughput screening.
Mammalian catechol-O-methyltransferases (COMT) are an important class of conjugative enzymes, which play a key role in the metabolism and inactivation of catechol neurotransmitters, catechol estrogens and a wide range of endobiotics and xenobiotics that bear the catechol group. Currently, COMT inhibitors are used in combination with levodopa for the treatment of Parkinson's disease in clinical practice. The crucial role of COMT in human health has raised great interest in the development of more practical assays for highly selective and sensitive detection of COMT activity in real samples, as well as for rapid screening and characterization of COMT inhibitors as drug candidates. This review summarizes recent advances in analytical methodologies for sensing COMT activity and their applications. Several lists of biochemical assays for measuring COMT activity, including the probe substrates, along with their analytical conditions and kinetic parameters, are presented. Finally, the challenges and future perspectives in the field, such as visualization of COMT activity in vivo and in situ, are highlighted. Collectively, this review article overviews the practical assays for measuring COMT activities in complex biological samples, which will strongly facilitate the investigations on the relevance of COMT to human diseases and promote the discovery of COMT inhibitors via high-throughput screening. (c) 2020 Xi'an Jiaotong University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据