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Anti-Parkinson drug biperiden inhibits enzyme acetylcholinesterase
Authors: Kostelník Adam | Čegan Alexander | Pohanka Miroslav
Year: 2017
Type of publication: článek v odborném periodiku
Name of source: Biomed Research International
Page from-to: "2532764-1"-"2532764-5"
Titles:
Language Name Abstract Keywords
cze Biperiden inhibuje enzym acetylcholinesterasu Biperiden je lék užívaný při léčbě Parkinsonovy nemoci. Funguje jako antagonista acetylcholinem aktivovaných muskarinových receptorů. Acetylcholinesterasa je enzym inhibovaný různým spektrem látek, nicméně zmínka o její interakci s biperidenem v literatuře chybí. Proto byla tato interakce prozkoumána a experimentální data byla doplněna o in-silico studii za využití SwissDock softwaru. Byl zjištěn mechanismus ihibice a spočítána inhibiční konstanta (1,11 mmol/l); interakce biperidenu s enzymem byla zjištěna na úrovni periferního anionického místa. Biperiden je velmi slabým inhibitorem acetylcholinesterasy, ale v budoucnu by tato sturkura mohla sloužit při výzkumu nových cholinesterasových inhibitorů. Acetylcholinesterasa; biperiden; inhibitor; docking
eng Anti-Parkinson drug biperiden inhibits enzyme acetylcholinesterase Biperiden is a drug used in Parkinson disease treatment. It acts as antagonist of muscarinic receptor activated by acetylcholine. Acetylcholinesterase is an enzyme inhibited by various compounds, however there has not been proposed evidence about interaction with biperiden molecule. Therefore, we investigated this interaction using standard Ellman´s assay and experimental data were completed with in-silico prediction by SwissDock docking software. We revealed inhibition mechanism and inhibition constant was calculated to be 1.11 mmol/l; interaction of biperiden occurs in peripheral anionic subsite. Biperiden appeared to be very weak inhibitor but it can serve as a leading structure in a pharmacological research. Acetylcholinesterase; biperiden; inhibitor; docking

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