A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor.

Abstract

Ligands targeting G protein-coupled receptors (GPCRs) are currently classified as either orthosteric, allosteric, or dualsteric/bitopic. Here, we introduce a new pharmacological concept for GPCR functional modulation: sequential receptor activation. A hallmark feature of this is a stepwise ligand binding mode with transient activation of a first receptor… (More)
DOI: 10.1016/j.chembiol.2016.02.014

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Cite this paper

@article{Grundmann2016AMM, title={A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor.}, author={Manuel Grundmann and Irina G. Tikhonova and Brian D. Hudson and Nicola J. Smith and Klaus Mohr and Trond Ulven and Graeme Milligan and Terry Kenakin and Evi Kostenis}, journal={Cell chemical biology}, year={2016}, volume={23 3}, pages={392-403} }