October 2022 Structural perspectives on the mechanism of signal activation, ligand selectivity and allosteric opportunities to examine the dynamic fluxes in the 3D architecture of the receptors, as the basis of ligand selectivity Constituent structural motifs cooperatively transform ligand selectivity into specific functions, thus

August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin important neurotransmitter that activates 12 different G protein-coupled receptors (GPCRs) through selective The structural basis for G protein subtype selectivity by these GPCRs remains elusive. that transmembrane helices TM5 and TM6 alternate lengths as a macro-switch to determine receptor's selectivity Together, these results present a common mechanism of Gs versus Gi protein coupling selectivity or promiscuity

therapeutic drugs have been developed to treat these diseases; however, they lack receptor subtype selectivity a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor in complex with a selective unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor subtype selectivity

Selection pressure analysis revealed that CCR4La, CCR4Lc, CCR12a1, and CCR12a2 underwent negative selection pressure, whereas CCR12b experienced positive selection pressure. Robust selection site detection methods identified that positive selected sites of CCR4La, CCR4Lc, CCR12a1 Similarly, the positive selected sites of CCR12b were also located in its extracellular regions. The accuracy of the pressure selected sites were also validated by molecular docking analysis.

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Illuminating Functional Selectivity

Committee Sponsors GPCR Retreat Program < Back to schedule Structure-based discovery of functionally selective Peter Gmeiner has been spokesman of the Research Training Group "Medicinal Chemistry of Selective GPCR