Article
Domains for activation and inactivation in G protein-coupled receptors--a mutational analysis of constitutive activity of the adenosine A2B receptor.
Biochemical pharmacology - 15 Nov 2014
Peeters Miriam C, Li Qilan, Elands Rachel, van Westen Gerard J P, Lenselink Eelke B, Müller Christa E, IJzerman Adriaan P
Abstract excerpt
G protein-coupled receptors (GPCRs) are a major drug target and can be activated by a range of stimuli, from photons to proteins. Most, if not all, GPCRs also display a basal level of biological response in the absence of such a stimulus. This level of so-called constitutive activity results from a delicate energy equilibrium that exists between the active and the inactive state of the receptor and is the first...
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