G protein–coupled receptors (GPCRs) are versatile molecular machines that regulate the majority of physiological responses to chemically diverse hormones and neurotransmitters. Recent breakthroughs in structural studies have advanced our understanding of GPCR signaling, particularly the selectivity of ligand recognition and receptor activation of G proteins.
This is a preview of subscription content, access via your institution
Relevant articles
Open Access articles citing this article.
-
Coevolution underlies GPCR-G protein selectivity and functionality
Scientific Reports Open Access 12 April 2021
-
Computational design and characterization of nanobody-derived peptides that stabilize the active conformation of the β2-adrenergic receptor (β2-AR)
Scientific Reports Open Access 12 November 2019
-
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Nature Communications Open Access 23 July 2019
Access options
Subscribe to this journal
Receive 12 print issues and online access
$259.00 per year
only $21.58 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
References
Bockaert, J. & Pin, J.P. EMBO J. 18, 1723–1729 (1999).
Schertler, G.F. Eye (Lond.) 12, 504–510 (1998).
Palczewski, K. et al. Science 289, 739–745 (2000).
Rasmussen, S.G. et al. Nature 450, 383–387 (2007).
Kobilka, B. & Schertler, G.F. Trends Pharmacol. Sci. 29, 79–83 (2008).
Rasmussen, S.G. et al. Nature 477, 549–555 (2011).
Rosenbaum, D.M. et al. Science 318, 1266–1273 (2007).
Jaakola, V.P. et al. Science 322, 1211–1217 (2008).
Hanson, M.A. et al. Science 335, 851–855 (2012).
Manglik, A. et al. Nature 485, 321–326 (2012).
Granier, S. et al. Nature 485, 400–404 (2012).
Wu, H. et al. Nature 485, 327–332 (2012).
Thompson, A.A. et al. Nature 485, 395–399 (2012).
Kruse, A.C. et al. Nature 482, 552–556 (2012).
Haga, K. et al. Nature 482, 547–551 (2012).
Dror, R.O. et al. Proc. Natl. Acad. Sci. USA 108, 18684–18689 (2011).
Lebon, G., Warne, T. & Tate, C.G. Curr. Opin. Struct. Biol. doi:10.1016/j.sbi.2012.03.007 (3 April 2012).
Rosenbaum, D.M. et al. Nature 469, 236–240 (2011).
Kahsai, A.W. et al. Nat. Chem. Biol. 7, 692–700 (2011).
Liu, J.J., Horst, R., Katritch, V., Stevens, R.C. & Wuthrich, K. Science 335, 1106–1110 (2012).
Rahmeh, R. et al. Proc. Natl. Acad. Sci. USA 109, 6733–6738 (2012).
Rajagopal, S., Rajagopal, K. & Lefkowitz, R.J. Nat. Rev. Drug Discov. 9, 373–386 (2010).
Wu, B. et al. Science 330, 1066–1071 (2010).
Bonacci, T.M. et al. Science 312, 443–446 (2006).
Kobilka, B.K. & Deupi, X. Trends Pharmacol. Sci. 28, 397–406 (2007).
Author information
Authors and Affiliations
Corresponding author
Ethics declarations
Competing interests
The authors declare no competing financial interests.
Rights and permissions
About this article
Cite this article
Granier, S., Kobilka, B. A new era of GPCR structural and chemical biology. Nat Chem Biol 8, 670–673 (2012). https://doi.org/10.1038/nchembio.1025
Published:
Issue Date:
DOI: https://doi.org/10.1038/nchembio.1025
This article is cited by
-
Coevolution underlies GPCR-G protein selectivity and functionality
Scientific Reports (2021)
-
Encoding mu-opioid receptor biased agonism with interaction fingerprints
Journal of Computer-Aided Molecular Design (2021)
-
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Nature Communications (2019)
-
Computational design and characterization of nanobody-derived peptides that stabilize the active conformation of the β2-adrenergic receptor (β2-AR)
Scientific Reports (2019)
-
Dual binding mode of “bitter sugars” to their human bitter taste receptor target
Scientific Reports (2019)