Creative Animodel is a leading contract research organization providing GPCRs services to meet the needs of drug discovery. Our experienced scientists and professional technical platforms enable us to deliver reliable results in a cost-efficient manner.
What Are GPCRs?
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR) constitute a large protein family of receptors. GPCRs can detect molecules outside the cell, activate internal signal transduction pathways and cellular responses. They involve a wide range of physiological processes, such as visual sense, gustatory sense, sense of smell, regulation of immune system activity and inflammation, as well as autonomic nervous system transmission. Because of their important functions, they are associated with diseases ranging from cardiovascular diseases, autoimmune diseases, inflammation, cancer, and diseases of the nervous system. In addition, GPCRs are one of the most popular drug targets for the reason that they can be modulated by small molecules, peptides, and proteins. It is reported that about 40% of drugs on the market are targeting GPCRs. And GPCR screening and profiling plays an important role in GPCR drug discovery.
Figure 1. GPCR signal transduction (Dolatshad N F, 2015)
GPCRs Services at Creative Animodel
We can offer binding assays and functional assays to meet the requirements of GPCR drug discovery. The combination of binding assays and functional assays can provide integrated information of a compound’s in vitro pharmacology.
• Binding assays.
GPCR binding assays can be used to detect interaction between GCPRs and their ligands or compounds. The binding assay is a cell-free method theoretically suitable for any GPCR screening without involving downstream signaling from the receptor. We provide various methods to conduct binding assays, such as radioligand binding assay, scintillation proximity assay (SPA) and time-resolved fluorescence resonance energy transfer (TR-FRET).
• Functional assays.
Through GPCR functional assays, we can detect the activity of target GPCR, and provide additional information on functional selectivity of candidate compounds. We can provide cell based assays covering multiple second messenger readouts and receptor internalization assays, such as cAMP assays, IP3/IP1 and Ca2+ assays, label-free cell based assays, as well as CTPyS assays.
• Abundant selections of binding and functional assays are provided to test the binding affinity and mechanisms of action (MOA) of compounds.
• Rapid turnaround time based on conducting assays and delivering results in a time-saving manner.
• Customized GPCR screening and profiling services are available depending on clients’ needs for GPCRs drug discovery.
• Our GPCR screening and profiling services include more than one hundred targets and cover all major GPCR classes’ receptors.
Creative Animodel provides a wide variety of GPCRs services. No matter what services you are looking for, we can provide all the GPCRs drug discovery solutions for you. If you have any questions or specific needs, please feel free to contact us.
1. Dolatshad N F, et al. G-protein coupled receptor signaling in pluripotent stem cell-derived cardiovascular cells: implications for disease modeling. Frontiers in cell and developmental biology, 2015, 3.
2. Ke N, et al.; Multidimensional GPCR profiling and screening using impedance-based label-free and real-time assay. G Protein-Coupled Receptor Screening Assays: Methods and Protocols, 2015: 215-226.