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Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy
- 1.0359734 - FGÚ 2012 RIV GB eng J - Journal Article
Jakubík, Jan - Janíčková, Helena - El-Fakahany, E. E. - Doležal, Vladimír
Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy.
British Journal of Pharmacology. Roč. 162, č. 5 (2011), s. 1029-1044. ISSN 0007-1188. E-ISSN 1476-5381
R&D Projects: GA ČR(CZ) GA305/09/0681; GA AV ČR(CZ) IAA500110703; GA MŠMT(CZ) LC554
Institutional research plan: CEZ:AV0Z50110509
Keywords : acetylcholine * muscarinic receptor * GDP
Subject RIV: FH - Neurology
Impact factor: 4.409, year: 2011
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
Permanent Link: http://hdl.handle.net/11104/0197462
Number of the records: 1