Molecular signatures of G-protein-coupled receptors
- PMID: 23407534
- DOI: 10.1038/nature11896
Molecular signatures of G-protein-coupled receptors
Abstract
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that sense signalling molecules such as hormones and neurotransmitters, and are the targets of several prescribed drugs. Recent exciting developments are providing unprecedented insights into the structure and function of several medically important GPCRs. Here, through a systematic analysis of high-resolution GPCR structures, we uncover a conserved network of non-covalent contacts that defines the GPCR fold. Furthermore, our comparative analysis reveals characteristic features of ligand binding and conformational changes during receptor activation. A holistic understanding that integrates molecular and systems biology of GPCRs holds promise for new therapeutics and personalized medicine.
Similar articles
-
Emerging opportunities for allosteric modulation of G-protein coupled receptors.Biochem Pharmacol. 2013 Jan 15;85(2):153-62. doi: 10.1016/j.bcp.2012.09.001. Epub 2012 Sep 11. Biochem Pharmacol. 2013. PMID: 22975406 Review.
-
Conformational complexity of G-protein-coupled receptors.Trends Pharmacol Sci. 2007 Aug;28(8):397-406. doi: 10.1016/j.tips.2007.06.003. Epub 2007 Jul 13. Trends Pharmacol Sci. 2007. PMID: 17629961 Review.
-
Emerging structural insights into biased GPCR signaling.Trends Biochem Sci. 2014 Dec;39(12):594-602. doi: 10.1016/j.tibs.2014.10.001. Epub 2014 Nov 4. Trends Biochem Sci. 2014. PMID: 25458114 Review.
-
G-protein-coupled receptor structure, ligand binding and activation as studied by solid-state NMR spectroscopy.Biochem J. 2013 Mar 15;450(3):443-57. doi: 10.1042/BJ20121644. Biochem J. 2013. PMID: 23445222 Review.
-
G protein-coupled receptors--recent advances.Acta Biochim Pol. 2012;59(4):515-29. Epub 2012 Dec 18. Acta Biochim Pol. 2012. PMID: 23251911 Free PMC article. Review.
Cited by
-
Active-state models of ternary GPCR complexes: determinants of selective receptor-G-protein coupling.PLoS One. 2013 Jun 24;8(6):e67244. doi: 10.1371/journal.pone.0067244. Print 2013. PLoS One. 2013. PMID: 23826246 Free PMC article.
-
What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands?Pharmacol Rev. 2015;67(1):198-213. doi: 10.1124/pr.114.009944. Pharmacol Rev. 2015. PMID: 25527701 Free PMC article. Review.
-
Generic GPCR residue numbers - aligning topology maps while minding the gaps.Trends Pharmacol Sci. 2015 Jan;36(1):22-31. doi: 10.1016/j.tips.2014.11.001. Epub 2014 Dec 22. Trends Pharmacol Sci. 2015. PMID: 25541108 Free PMC article. Review.
-
G-protein coupled receptors: advances in simulation and drug discovery.Curr Opin Struct Biol. 2016 Dec;41:83-89. doi: 10.1016/j.sbi.2016.06.008. Epub 2016 Jun 22. Curr Opin Struct Biol. 2016. PMID: 27344006 Free PMC article. Review.
-
Generation of a Polyclonal Antibody against the Mouse Metal Transporter ZIP8.Antibodies (Basel). 2021 Apr 21;10(2):16. doi: 10.3390/antib10020016. Antibodies (Basel). 2021. PMID: 33919173 Free PMC article.
References
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources