Special

G protein–coupled receptors

G protein-coupled receptors (GPCRs) are membrane proteins that are involved in a broad range of biological processes, and a large number of clinically used drugs elicit their biological effect(s) via a GPCR. Structural information about GPCRs was very limited until 2007, and papers describing new GPCR structures and previously unseen conformational states have dramatically increased in the past few years. In this online special, we present a selection of recently published Nature papers that involve the structures of various GPCRs. Understanding the conformational changes that occur in these proteins when a ligand binds to and activates the receptor should facilitate the development of potential drugs with fewer side effects and more favorable pharmacological properties.

Credit: Kobilka et al.

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Molecular signatures of G-protein-coupled receptors

Venkatakrishnan et al.

Nature 494, 185-194 ( 14 February 2013 )
High-resolution crystal structure of human protease-activated receptor 1

Zhang C et al.

Nature 492, 387-392 ( 20 December 2012 )
NOBEL 2012 Chemistry: Studies of a ubiquitous receptor family

Bryan L. Roth & Fiona H. Marshall

Nature 492, 57 ( 06 December 2012 )
Structure of the chemokine receptor CXCR1 in phospholipid bilayers

Park SH et al.

Nature 491, 779-783 ( 29 November 2012 )
Structure of the agonist-bound neurotensin receptor

White JF et al.

Nature 490, 508-513 ( 25 October 2012 )
Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

Manglik A et al.

Nature 485, 321-326 ( 17 May 2012 )
Structure of the human κ-opioid receptor in complex with JDTic

Wu H et al.

Nature 485, 327-332 ( 17 May 2012 )
Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic

Thompson AA et al.

Nature 485, 395-399 ( 17 May 2012 )
Structure of the δ-opioid receptor bound to naltrindole

Granier S et al.

Nature 485, 400-404 ( 17 May 2012 )
Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

Haga K et al.

Nature 482, 547-551 ( 23 February 2012 )
Structure and dynamics of the M3 muscarinic acetylcholine receptor

Kruse AC et al.

Nature 482, 552-556 ( 23 February 2012 )
G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody

Hino T et al.

Nature 482, 237-240 ( 29 January 2012 )
Crystal structure of the β2 adrenergic receptor-Gs protein complex

Rasmussen SGF et al.

Nature 477, 549-555 ( 29 September 2011 )
Conformational changes in the G protein Gs induced by the β2 adrenergic receptor

Chung KY et al.

Nature 477, 611-615 ( 29 September 2011 )
Structure of the human histamine H1 receptor complex with doxepin

Shimamura T et al.

Nature 475, 65-70 ( 07 July 2011 )
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Lebon G et al.

Nature 474, 521-525 ( 23 June 2011 )
Crystal structure of metarhodopsin II

Choe HW et al.

Nature 471, 651-655 ( 31 March 2011 )
The structural basis of agonist-induced activation in constitutively active rhodopsin

Standfuss J et al.

Nature 471, 656-660 ( 31 March 2011 )
The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

Warne T et al.

Nature 469, 241-244 ( 13 January 2011 )
Structure and function of an irreversible agonist-β2 adrenoceptor complex

Rosenbaum DM et al.

Nature 469, 236-240 ( 13 January 2011 )
Structure of a nanobody-stabilized active state of the β2 adrenoceptor

Rasmussen SG et al.

Nature 469, 175-180 ( 13 January 2011 )
Tracking G-protein-coupled receptor activation using genetically encoded infrared probes

Ye S et al.

Nature 464, 1386-1389 ( 29 April 2010 )
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

Bokoch MP et al.

Nature 463, 108-112 ( 07 January 2010 )

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Nobel work boosts drug development

Richard Van Noorden

Nature 490, 320 ( 18 October 2012 )
Opioid receptors revealed

Buchen L

Nature 483, 383 ( 21 March 2012 )
Cell signalling: It's all about the structure

Buchen L

Nature 476, 387-390 ( 25 August 2011 )
Cell signalling caught in the act

Buchen L

Nature 475, 273-274 ( 19 July 2011 )
Structural biology: The gatekeepers revealed

Baker M

Nature 465, 823-826 ( 10 June 2010 )

G protein–coupled receptors

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