Journal ArticleDOI
Structure and Function of G Protein Coupled Receptors
Jelveh Lameh,Ric I. Cone,Sadaaki Maeda,Mohan Philip,Maithe Corbani,Laszlo Nadasdi,J. Ramachandran,Graham M. Smith,Wolfgang Sadee +8 more
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TLDR
This review summarizes the current knowledge of the molecular mechanisms by which the GPC-Rs activate second messenger systems, and it addresses their regulation and structure.Abstract:
The G protein coupled receptors (GPC-Rs) comprise a large superfamily of genes encoding numerous receptors which all show common structural features, e.g., seven putative membrane spanning domains. Their biological functions are extremely diverse, ranging from vision and olfaction to neuronal and endocrine signaling. The GPC-Rs couple via multiple G proteins to a growing number of recognized second messenger pathway, e.g., cAMP and phosphatidyl inositol turnover. This review summarizes our current knowledge of the molecular mechanisms by which the GPC-Rs activate second messenger systems, and it addresses their regulation and structure.read more
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Journal ArticleDOI
Structure of a nanobody-stabilized active state of the β2 adrenoceptor
Søren G. F. Rasmussen,Hee Jung Choi,Juan Jose Fung,Els Pardon,Paola Casarosa,Pil Seok Chae,Brian T. DeVree,Daniel M. Rosenbaum,Foon Sun Thian,Tong Sun Kobilka,Andreas Schnapp,Ingo Konetzki,Roger K. Sunahara,Samuel H. Gellman,Alexander Pautsch,Jan Steyaert,William I. Weis,Brian K. Kobilka +17 more
TL;DR: A camelid antibody fragment to the human β2 adrenergic receptor is generated, and an agonist-bound, active-state crystal structure of the receptor-nanobody complex is obtained, providing insights into the process of agonist binding and activation.
Journal ArticleDOI
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update
TL;DR: In the 10 years since the previous International Union of Basic and Clinical Pharmacology report on the nomenclature and classification of adenosine receptors, no developments have led to major changes in the recommendations, but there have been so many other developments that an update is needed.
Journal ArticleDOI
G Protein-Coupled Receptor Allosterism and Complexing
TL;DR: It is proposed that the study of allosteric phenomena will become of progressively greater import to the drug discovery process due to the advent of newer and more sensitive GPCR screening technologies.
Journal ArticleDOI
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation
Guillaume Lebon,Tony Warne,Patricia C. Edwards,K.A. Bennett,Christopher J. Langmead,Andrew G. W. Leslie,Christopher G. Tate +6 more
TL;DR: Two crystal structures of the thermostabilized human adenosine A2A receptor bound to its endogenous agonistAdenosine and the synthetic agonist NECA are presented, indicating that the contraction of the ligand-binding pocket caused by the inward motion of helices 3, 5 and 7 may be a common feature in the activation of all GPCRs.
Journal ArticleDOI
Structure and function of an irreversible agonist-β2 adrenoceptor complex
Daniel M. Rosenbaum,Cheng Zhang,Joseph A. Lyons,Joseph A. Lyons,Ralph Holl,David Aragão,Daniel H. Arlow,Sã̧ren G F Rasmussen,Hee Jung Choi,Brian T. DeVree,Roger K. Sunahara,Pil Seok Chae,Samuel H. Gellman,Ron O. Dror,David E. Shaw,William I. Weis,Martin Caffrey,Peter Gmeiner,Brian K. Kobilka +18 more
TL;DR: A covalent agonist-bound β2AR–T4L fusion protein is designed that can be covalently tethered to a specific site on the receptor through a disulphide bond, and is capable of activating a heterotrimeric G protein.
References
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