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G PROTEIN-COUPLED RECEPTORS
G protein-coupled receptors (GPCRs) are the largest family of cell surface communicating molecules. They facilitate diverse extracellular signals and, therefore, play a crucial role in numerous physiological processes and diseases. Subsequently, GPCRs have become drug targets for many major diseases. To date, however, only a small proportion of GPCRs have been investigated as targets, so this area still shows great potential in combatting many other diseases. The March 2012 issue contains a special feature on GPCRs including articles by leading experts on GPCR structures, biology, diseases, and drug discovery. Further background information on this important topic is available through the accompanying web focus which links to related articles from across Nature Publishing Group.
Original Articles
A GPCR/secretase complex regulates β- and γ-secretase specificity for Aβ production and contributes to AD pathogenesis
Lin Teng, Jian Zhao, Feifei Wang, Lan Ma and Gang Pei
Cell Research (2010) 20: 138–153; doi:10.1038/cr.2010.3
GPR55 regulates cannabinoid 2 receptor-mediated responses in human neutrophils
Nariman A B Balenga, Elma Aflaki, Julia Kargl, Wolfgang Platzer, Ralf Schröder, Stefanie Blättermann, Evi Kostenis, Andrew J Brown, Akos Heinemann & Maria Waldhoer
Cell Research (2011) 21: 1452–1469; doi:10.1038/cr.2011.60
Classification of 5-HT1A receptor agonists and antagonists using GA-SVM method
Xue-lian Zhu, Hai-yan Cai, Zhi-jian Xu, Yong Wang, He-yao Wang, Ao Zhang & Wei-liang Zhu
Acta Pharmacologica Sinica (2011) 32: 1424–1430; doi:10.1038/aps.2011.112
Research Article
Pathway-selective suppression of chemokine receptor signaling in B cells by LPS through downregulation of PLC-β2
Aiko-Konno Shirakawa, Fang Liao, Hongwei H Zhang, Michael N Hedrick, Satya P Singh, Dianqing Wu & Joshua M Farber
Cellular & Molecular Immunology (2010) 7: 428–439; doi:10.1038/cmi.2010.46
Reviews
Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors
Dong-Soon Im
Acta Pharmacologica Sinica (2010) 31: 1213–1222; doi:10.1038/aps.2011.112
Articles
Sub-picomolar relaxin signalling by a pre-assembled RXFP1, AKAP79, AC2, β-arrestin 2, PDE4D3 complex
Michelle L Halls & Dermot M F Cooper
The EMBO Journal (2010) 29: 2772–2787; doi:10.1038/emboj.2010.168
Molecular basis for activation of G protein-coupled receptor kinases
Cassandra A Boguth, Puja Singh, Chih-chin Huang & John J G Tesmer
The EMBO Journal (2010) 29: 3249–3259; doi:10.1038/emboj.2010.206
Molecular organization and dynamics of the melatonin MT1 receptor/RGS20/Gi protein complex reveal asymmetry of receptor dimers for RGS and Gi coupling
Pascal Maurice, Avais M Daulat, Rostislav Turecek, Klara Ivankova-Susankova, Francesco Zamponi, Maud Kamal, Nathalie Clement, Jean-Luc Guillaume, Bernhard Bettler, Céline Gal&egreve;s, Philippe Delagrange & Ralf Jockers
The EMBO Journal (2010) 29: 3646–3659; doi:10.1038/emboj.2010.236
Crystal structure of the β2 adrenergic receptor–Gs protein complex
Søren G. F. Rasmussen, Brian T. DeVree, Yaozhong Zou, Andrew C. Kruse, Ka Young Chung, Tong Sun Kobilka, Foon Sun Thian, Pil Seok Chae, Els Pardon, Diane Calinski, Jesper M. Mathiesen, Syed T. A. Shah, Joseph A. Lyons, Martin Caffrey, Samuel H. Gellman, Jan Steyaert, Georgios Skiniotis, William I. Weis, Roger K. Sunahara & Brian K. Kobilka.
Nature (2011) 474: 549–555; doi:10.1038/nature10361
Letters
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation
Guillaume Lebon, Tony Warne, Patricia C. Edwards, Kirstie Bennett, Christopher J. Langmead, Andrew G. W. Leslie & Christopher G. Tate
Nature (2011) 474: 521–525; doi:10.1038/nature10136
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