Improved GPCR ligands from nanobody tethering

Extracting Common Substructures of GPCR Ligands

G-protein coupled receptor (GPCR) proteins are transmembrane receptor proteins which sense outer signals and activate various signaling pathways inside the cell causing different cellular responses. They have a wide range of sensory functions including sensing light, olfaction, hormone reception and neurotransmission. They exist in every tissue of our body and play important roles in regulation...

Tethering functional ligands onto shell of ultrasound active polymeric microbubbles.

Hollow (air-filled) microparticles, i.e., microbubbles, provide a promising novel vehicle for both local delivery of therapeutic agents and simultaneous diagnostic ultrasound echo investigations. In this paper, we describe the synthetic routes for decorating the polymeric shell of a poly(vinyl alcohol)-based microbubble with low and high molecular weight ligands with pharmacological relevance. ...

Screening for GPCR Ligands Using Surface Plasmon Resonance

G-protein coupled receptors (GPCRs) are a class of drug targets of primary importance. However, receptor assays are based on measurement of either ligand displacement or downstream functional responses, rather than direct observation of ligand binding. Issues of allosteric modulation, probe dependence, and functional selectivity create challenges in selecting suitable assays formats. Therefore,...

GPCRdb in 2018: adding GPCR structure models and ligands

G protein-coupled receptors are the most abundant mediators of both human signalling processes and therapeutic effects. Herein, we report GPCRome-wide homology models of unprecedented quality, and roughly 150 000 GPCR ligands with data on biological activities and commercial availability. Based on the strategy of 'Less model - more Xtal', each model exploits both a main template and alternative...

GPCR targeted library design: novel dopamine D3 receptor ligands.