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Cell. 2017 Jul 27;170(3):414-427. doi: 10.1016/j.cell.2017.07.009.

How Ligands Illuminate GPCR Molecular Pharmacology.

Author information

1
Department of Pharmacology and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC 27514, USA.
2
Departments of Biological Sciences and Chemistry, Bridge Institute, University of Southern California, Los Angeles, CA 90089, USA.
3
Department of Pharmacology and Division of Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC 27514, USA. Electronic address: bryan_roth@med.unc.edu.

Abstract

G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and synthetic ligands, represent the largest family of druggable targets in the human genome. Recent structural and molecular studies have both transformed and expanded classical concepts of receptor pharmacology and have begun to illuminate the distinct mechanisms by which structurally, chemically, and functionally diverse ligands modulate GPCR function. These molecular insights into ligand engagement and action have enabled new computational methods and accelerated the discovery of novel ligands and tool compounds, especially for understudied and orphan GPCRs. These advances promise to streamline the development of GPCR-targeted medications.

PMID:
28753422
PMCID:
PMC5560499
DOI:
10.1016/j.cell.2017.07.009
[Indexed for MEDLINE]
Free PMC Article

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