Jillian N Pearring, William J Spencer ... Vadim Y Arshavsky
Rather than relying on intrinsic intracellular targeting information, the key phototransduction enzyme guanylate cyclase 1 is delivered to the photosensory cilium with the visual pigment rhodopsin.
A comprehensive approach to prediction of stabilizing mutations in G-protein coupled receptors yields high hit rate and crystal structures of 5HT2C in both active and inactive states.
Hydrogen-Deuterium exchange experiments show that Ric-8A induces similar dynamic changes in the structure of Gα as G protein-coupled receptors, yet protects a larger surface of the nucleotide-binding Ras domain.
Contrary to previous findings, class A GPCRs share a common activation pathway that directly links ligand binding to G-protein activation, as revealed by novel quantitative analysis.
Ligand-specific-induced conformations of M3 muscarinic receptors reveal similar requirements for G protein-coupled receptor kinase 2 and Gq protein binding, whereas arrestin3 binding is mediated by distinct receptor conformations.
Qian Li, Yaw Tachie-Baffour ... Stephen D Liberles
Fish trace amine-associated receptors evolved a novel structural motif that enables the detection of chemically diverse amine odors in a non-canonical 'inverted' orientation.
A viral heliorhodopsin from Emiliania huxleyi virus 202 (V2HeR3) is a light-activated proton transporter, which has the potential to depolarize the host cells by light, possibly to overcome the host defense mechanisms or to prevent superinfection.
Alexander S Hauser, Charlotte Avet ... David E Gloriam
The GPCR-G protein coupling map and selectivity insights will catalyze advances in receptor research, cellular signaling, and drug discovery exploiting G protein signaling bias to design safer drugs.
Linking deep mutational scanning with engineered transcriptional reporters in human cell lines establishes a generalizable method for exploring pharmacogenomics, structure, and function across broad classes of drug receptors.