The two-state model of receptor activation

On the nature of allosteric transitions: A plausible model

Jacques Monod, Jeffries Wyman, Jean‐Pierre Changeux · Journal of Molecular Biology · 1965 · 8.9K citations

Life Sciences, Biochemistry, Molecular Biology +10

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

Philippe Samama, Susanna Cotecchia, Tommaso Costa et al. · Journal of Biological Chemistry · 1993 · 1.3K citations · Full text

Life Sciences, Molecular Biology, Pharmacology +17

Inverse agonist activity of beta-adrenergic antagonists.

Peter Chidiac, Terence E. Hébert, Manon Valiquette et al. · Molecular Pharmacology · 1994 · 373 citations

Medicine, Pharmacology, Cell Signaling +13

Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand.

Tommaso Costa, Yukiko Ogino, Peter J. Munson et al. · Molecular Pharmacology · 1992 · 242 citations

Medicine, Molecular Biology, Pharmacology +17

Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor.

Philippe Samama, Gang Pei, Tommaso Costa et al. · Molecular Pharmacology · 1994 · 238 citations

Life Sciences, Biochemistry, Pharmacology +17