The March 2012 issue of APS contains nine exciting reviews that cover a broad scope of GPCR structures, biology, disease, and drug discovery.
Four reviews are dedicated to GPCR structures.
ZHOU et al review the signaling mechanisms gained from rhodopsin structures and compare these mechanisms to other members of Class A GPCRs, most notably β2-adrenergic receptor (β2AR).
XU et al and LIU et al groups review the structures and ligand binding mechanisms of Class B and Class C GPCRs, respectively.
ZHAO et al provide a thorough review on the technology development in various stages of structure determination, including protein expression, purification, crystallization, and X-ray diffraction.
Five reviews are focused on GPCR biology, diseases, and drug discovery.
XIAO et al review the signaling mechanisms by β-adrenergic receptor subtypes that provide a basis for developing selective biased β2 agonists for the treatment of heart failure.
YE et al review the role of GPCRs in inflammation processes from chemotaxisis to transcriptional regulation of inflammation programs.
MAGGIOLINI et al provide a systematic review on the relationship of cancers with various subfamilies of GPCRs, which may serve as the basis for developing novel pharmacological interventions for cancers.
LIU et al provide a thorough review on different class of orphan nuclear receptors, their functions, and possible strategies for identification of endogenous ligands.
XIE et al provide a comprehensive review on methods of GPCR drug discovery, including various ligand binding and cell-based functional assays, many of which are tool kits for basic research as well as drug discovery for GPCRs.
For more information please visit http://www.nature.com/aps/focus/GPCR