Počet záznamů: 1

Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy

  1. 1.
    0359734 - FGU-C 2012 RIV GB eng J - Článek v odborném periodiku
    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
    Grant CEP: GA ČR(CZ) GA305/09/0681; GA AV ČR(CZ) IAA500110703; GA MŠk(CZ) LC554
    Výzkumný záměr: CEZ:AV0Z50110509
    Klíčová slova: acetylcholine * muscarinic receptor * GDP
    Kód oboru RIV: FH - Neurologie, neurochirurgie, neurovědy
    Impakt faktor: 4.409, rok: 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
    Trvalý link: http://hdl.handle.net/11104/0197462