Role of post-translational modifications on structure, function and pharmacology of class C G protein-coupled receptors

Lenea Nørskov-Lauritsen; Hans Bräuner-Osborne

doi:10.1016/j.ejphar.2015.05.015

Role of post-translational modifications on structure, function and pharmacology of class C G protein-coupled receptors

Eur J Pharmacol. 2015 Sep 15;763(Pt B):233-40. doi: 10.1016/j.ejphar.2015.05.015. Epub 2015 May 14.

Authors

Lenea Nørskov-Lauritsen¹, Hans Bräuner-Osborne²

Affiliations

¹ Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Denmark.
² Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Denmark. Electronic address: hbo@sund.ku.dk.

PMID: 25981296
DOI: 10.1016/j.ejphar.2015.05.015

Abstract

G protein-coupled receptors are divided into three classes (A, B and C) based on homology of their seven transmembrane domains. Class C is the smallest class with 22 human receptor subtypes including eight metabotropic glutamate (mGlu1-8) receptors, two GABAB receptors (GABAB1 and GABAB2), three taste receptors (T1R1-3), one calcium-sensing (CaS) receptor, one GPCR, class C, group 6, subtype A (GPRC6) receptor, and seven orphan receptors. G protein-coupled receptors undergo a number of post-translational modifications, which regulate their structure, function and/or pharmacology. Here, we review the existence of post-translational modifications in class C G protein-coupled receptors and their regulatory roles, with particular focus on glycosylation, phosphorylation, ubiquitination, SUMOylation, disulphide bonding and lipidation.

Keywords: CaSR; GPRC6A; Glycosylation; Palmitoylation; Phosphorylation; Post-translational modifications; Ubiquitination; mGluR.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Amino Acid Sequence
Animals
Humans
Molecular Sequence Data
Pharmacology / methods*
Protein Processing, Post-Translational*
Receptors, G-Protein-Coupled / chemistry*
Receptors, G-Protein-Coupled / metabolism*

Substances

Receptors, G-Protein-Coupled