GPCR Drug Discovery Assays and Products
Membrane proteins are the most successful class of therapeutic targets. Creative Biolabs has developed a comprehensive collection of membrane protein in vitro assays for drug discovery that cover most membrane protein targets.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
The most extensively researched therapeutic targets are G protein-coupled receptors (GPCRs), partly because of their important role in human pathophysiology and their pharmacological tractability. The number of biological medicines, allosteric modulators, and biased agonists has increased. There are presently over 320 compounds in clinical studies, of which 36% target 64 potentially new GPCR sites without an authorized medication. While other illnesses of the central nervous system continue to be heavily represented, diabetes, obesity, and Alzheimer's disease now account for the majority of disease indications for GPCR modulators.
Fig.1 Established and clinical trial GPCR drug targets. (Hauser, et al., 2017)
To meet the needs of GPCR drug discovery, Creative Biolabs can provide a wide variety of related assays and products:
According to their sequence and function, GPCRs are divided into six groups: Class A, rhodopsin-like receptors, Class B, secretin receptors, Class C, metabotropic glutamate receptors, Class D, fungal mating pheromone receptors, Class E, and Class F, frizzled and smoothened receptors. In order to assess the therapeutic effects of your candidate against the membrane protein targets, Creative Biolabs provides a wide variety of GPCR in vitro assays.
Creative Biolabs provides a range of GPCR assay kits to satisfy the diverse needs of your drug development programs. These detection reagents can be applied to a variety of tasks, such as translocation, compound-protein binding, second messenger assays, and protein-protein interactions that take place within cells.
To more fully understand the mechanisms and activities of GPCRs as well as innovative GPCR-related pharmacological therapies, GPCR cell lines are artificially created to express GPCRs in a stable manner. GPCR signaling pathways, GPCR agonists and antagonists, and chemical profiles can all be studied using measurements of GPCR proteins.
While HTS aids in automating research and accelerating development time, membrane ligand binding assays enable us to observe how a ligand or novel synthetic chemical interacts with a target protein and evaluate the affinity and kinetics of those interactions.
Creative Biolabs has developed a comprehensive list of membrane protein tools to support the development of antibodies and other therapeutics. We are dedicated to bringing more value to our clients by providing stock products, more technical resources and custom protein production services.
Orphan Receptors
Several orphan GPCRs that lack endogenous ligands are now being tested in clinical studies. The leucine-rich repeat-containing G protein-coupled receptors 4 and 5 (LGR4/5) for the treatment of gastrointestinal disease, the orphan GPCR GPR35 for the treatment of an allergic inflammatory condition, the orphan GPCR GPR55 as an antispasmodic target, the orphan GPCR proto-oncogene Mas (MAS) for the treatment of thrombocytopenia, and the orphan GPCR GPR84 for the treatment of ulcerative colitis are just This suggests that despite our inadequate understanding of the endogenous ligand and/or signaling system, drug research can continue to proceed and even advance.
Reference
- Hauser, A.S.; et al. Trends in GPCR drug discovery: new agents, targets and indications. Nature reviews Drug discovery. 2017, 16(12): 829-842.
