Positive effects of allosteric modulators on the binding properties and the function of muscarinic acetylcholine receptors.
Data are reviewed indicating that allosteric modulators can enhance the affinities of muscarinic receptors for their antagonists and agonists, that the enhancement of the affinity for agonists is relevant functionally, and that the allosterically induced conformational change also affects the interaction between the receptors and the G proteins.
Tucek
S
S
Institute of Physiology AV CR, Prague, Czech Republic.
Jakubík
J
J
Dolezal
V
V
el-Fakahany
E E
EE
D000494:Allosteric Regulation; D000818:Animals; D001665:Binding Sites; D019204:GTP-Binding Proteins / Q000378:metabolism; D018721:Muscarinic Agonists / Q000494:pharmacology*; D018727:Muscarinic Antagonists / Q000494:pharmacology*; D011487:Protein Conformation; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000378:metabolism
D018721:Muscarinic Agonists; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D019204:GTP-Binding Proteins