By comparing ligand-free G protein–coupled receptor (GPCR) structures with those of receptors bound to inverse agonists, agonists and signaling effectors, two recent papers refine the

understanding of GPCR activation. One group also reported the oligomeric assembly of the β1 adrenergic receptor in its ligand-free form, raising the question of the role of oligomers in

receptor activation. Access through your institution Buy or subscribe This is a preview of subscription content, access via your institution RELEVANT ARTICLES Open Access articles citing

this article. * UNDERSTANDING THE MOLECULAR BASIS OF AGONIST/ANTAGONIST MECHANISM OF HUMAN MU OPIOID RECEPTOR THROUGH GAUSSIAN ACCELERATED MOLECULAR DYNAMICS METHOD * Yeng-Tseng Wang *  

Subscribe to this journal Receive 12 print issues and online access $209.00 per year only $17.42 per issue Learn more Buy this article * Purchase on SpringerLink * Instant access to full

article PDF Buy now Prices may be subject to local taxes which are calculated during checkout ADDITIONAL ACCESS OPTIONS: * Log in * Learn about institutional subscriptions * Read our FAQs *

Contact customer support REFERENCES * Audet, M. & Bouvier, M. _Cell_ 151, 14–23 (2012). Article  CAS  Google Scholar  * Huang, J., Chen, S., Zhang, J.J. & Huang, X.Y. _Nat. Struct.

Mol. Biol._ 20, 419–425 (2013). Article  CAS  Google Scholar  * Warne, T. et al. _Nature_ 454, 486–491 (2008). Article  CAS  Google Scholar  * Warne, T. et al. _Nature_ 469, 241–244 (2011).

Article  CAS  Google Scholar  * Scheerer, P. et al. _Nature_ 455, 497–502 (2008). Article  CAS  Google Scholar  * Rasmussen, S.G. et al. _Nature_ 469, 175–180 (2011). Article  CAS  Google

Scholar  * Moukhametzianov, R. et al. _Proc. Natl. Acad. Sci. USA_ 108, 8228–8232 (2011). Article  CAS  Google Scholar  * Nygaard, R. et al. _Cell_ 152, 532–542 (2013). Article  CAS  Google

Scholar  * Galandrin, S., Oligny-Longpre, G. & Bouvier, M. _Trends Pharmacol. Sci._ 28, 423–430 (2007). Article  CAS  Google Scholar  * Rajagopal, S., Rajagopal, K. & Lefkowitz, R.J.

_Nat. Rev. Drug Discov._ 9, 373–386 (2010). Article  CAS  Google Scholar  * Vaidehi, N. & Kenakin, T. _Curr. Opin. Pharmacol._ 10, 775–781 (2010). Article  CAS  Google Scholar  *

Bulenger, S., Marullo, S. & Bouvier, M. _Trends Pharmacol. Sci._ 26, 131–137 (2005). Article  CAS  Google Scholar  * Smith, N.J. & Milligan, G. _Pharmacol. Rev._ 62, 701–725 (2010).

Article  CAS  Google Scholar  * Fotiadis, D. et al. _Curr. Opin. Struct. Biol._ 16, 252–259 (2006). Article  CAS  Google Scholar  * Wu, B. et al. _Science_ 330, 1066–1071 (2010). Article 

CAS  Google Scholar  * Manglik, A. et al. _Nature_ 485, 321–326 (2012). Article  CAS  Google Scholar  * Wu, H. et al. _Nature_ 485, 327–332 (2012). Article  CAS  Google Scholar  * Pin, J.P.

et al. _J. Physiol. (Lond.)_ 587, 5337–5344 (2009). Article  CAS  Google Scholar  * Whorton, M.R. et al. _Proc. Natl. Acad. Sci. USA_ 104, 7682–7687 (2007). Article  CAS  Google Scholar  *

Fung, J.J. et al. _EMBO J._ 28, 3315–3328 (2009). Article  CAS  Google Scholar  Download references AUTHOR INFORMATION AUTHORS AND AFFILIATIONS * Michel Bouvier is at the Department of

Biochemistry, Institute for Research in Immunology and Cancer, Université de Montréal, Montréal, Québec, Canada., Michel Bouvier Authors * Michel Bouvier View author publications You can

also search for this author inPubMed Google Scholar CORRESPONDING AUTHOR Correspondence to Michel Bouvier. ETHICS DECLARATIONS COMPETING INTERESTS The author declares no competing financial

interests. RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Bouvier, M. Unraveling the structural basis of GPCR activation and inactivation. _Nat Struct

Mol Biol_ 20, 539–541 (2013). https://doi.org/10.1038/nsmb.2584 Download citation * Published: 06 May 2013 * Issue Date: May 2013 * DOI: https://doi.org/10.1038/nsmb.2584 SHARE THIS ARTICLE

Anyone you share the following link with will be able to read this content: Get shareable link Sorry, a shareable link is not currently available for this article. Copy to clipboard Provided

by the Springer Nature SharedIt content-sharing initiative