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Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy
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SYSNO ASEP 0359734 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy Author(s) Jakubík, Jan (FGU-C) RID, ORCID
Janíčková, Helena (FGU-C) RID, ORCID, SAI
El-Fakahany, E. E. (US)
Doležal, Vladimír (FGU-C) RID, ORCIDSource Title British Journal of Pharmacology. - : Wiley - ISSN 0007-1188
Roč. 162, č. 5 (2011), s. 1029-1044Number of pages 16 s. Language eng - English Country GB - United Kingdom Keywords acetylcholine ; muscarinic receptor ; GDP Subject RIV FH - Neurology R&D Projects GA305/09/0681 GA ČR - Czech Science Foundation (CSF) IAA500110703 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) LC554 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z50110509 - FGU-C (2005-2011) UT WOS 000286668500003 DOI 10.1111/j.1476-5381.2010.01081.x Annotation Our findings suggest the existence of a low-affinity agonist-receptor conformation complexed with GDP-liganded G-protein. Also the negative cooperativity between GDP and agonist binding at the receptor/G-protein complex determines agonist efficacy. GDP binding reveals differences in action of agonists versus inverse agonists as well as differences in activation of Gi/o versus Gs/olf G-proteins that are not identified by conventional GTPalphaS binding Workplace Institute of Physiology Contact Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Year of Publishing 2012
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