The Assay Development Core is currently focused on establishing functional assays as well as searching for novel small molecule ligands of human G protein coupled receptors (GPCRs).
PCRs, also known as seven transmembrane domain receptors, are the largest and most diverse family of membrane receptors in eukaryotes. Over 40% of approved drugs on market target GPCRs, and therefore finding novel ligands for GPCRs remains a hot therapeutic topic.
In order to assist the needs of research groups, the assay development core has validated functional assays for several GPCRs. We currently provide assays to evaluate GPCR-related downstream signalling pathways, either by monitoring G protein related secondary messengers such as cAMP, IP1 and calcium flux, or by β-arrestin recruitment.
Another area of interest is to screen and quantify potential binders such as small molecules and antibodies of GPCRs. For affinity measurements, surface plasmon resonance (SPR) and fluorescent based flow cytometry are applied to various GPCRs. For novel ligand screening, a thermo shift assay is widely applied to search for molecules that can stabilize GPCRs for crystallization purposes. Combining with a liquid handling system, all functional assays can also be used for ligand screening.