Fundamental difference between the molecular interactions of agonists and antagonists with the beta-adrenergic receptor
Weiland, G.A.; Minneman, K.P.; Molinoff, P.B.
Nature 281(5727): 114-117
1979
ISSN/ISBN: 0028-0836 PMID: 38405 Document Number: 147875
Antagonist binding to the beta-adrenergic receptor is largely entropy driven, with only a small enthalpy component. The binding of agonists, on the other hand, is associated with a large decrease in enthalpy which permits a highly unfavourable decrease in entropy. The thermodynamic differences between the binding of agonists and antagonists may provide new insights into the molecular basis for hormone stimulation of adenylate cyclase activity.