PMID: 38405Sep 13, 1979

Fundamental difference between the molecular interactions of agonists and antagonists with the beta-adrenergic receptor

Nature
G A WeilandP B Molinoff

Abstract

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.

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Related Concepts

Thermodynamics
Adrenergic beta-Agonists
Beta-adrenergic receptor
Meleagridinae
Norepinephrine Receptors
Red Cell Ghost
Adenylate Cyclase
Ligands
Enzyme Activation
Adrenergic beta-Antagonists

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