G protein-coupled receptor (GPCR) membrane proteins

G protein-coupled receptors (GPCRs) are the largest group of membrane proteins. GPCRs' primary function is to convert a wide range of extracellular stimuli, including biogenic amines, peptides, hormones, neurotransmitters, ions, odorants, and photons, into intracellular signals that control a variety of physiological processes such as cell metabolism, differentiation, growth, neurotransmission, and sensory perception.

GPCRs have been linked to a wide range of disorders, including type 2 diabetes mellitus (T2DM), obesity, depression, cancer, Alzheimer’s disease, and others. As a result, GPCRs have emerged as the most effective drug target class for treating a wide range of diseases.

Structure of GPCRs

GPCRs have a common molecular structure of seven transmembrane alpha helices, which divide the receptor into the extracellular N-terminus, intracellular C-terminus, three extracellular loops, and three intracellular loops.

The extracellular ring comprises two highly conserved cysteine residues that create disulfide bonds to maintain the receptor’s spatial organization. The intracellular loop has a G protein binding site.

Schematic diagram of the classic GPCRs. Image Credit: ACROBiosystems Inc.

ACROBiosystems assists in the development of targeted GPCRs antibodies

Due to the restricted extracellular exposure of the GPCR target, poor cell surface expression, protein aggregation, and other variables, it is extremely difficult to generate biologically active soluble GPCR antigens. To develop new drugs, the whole structure that guarantees the GPCR antigen’s natural conformation is crucial.

Full-length GPCR proteins, such as GPRC5D, CXCR4, CCR5, and CCR8, are available from ACROBiosystems through specifically designed platform solutions of VLP, Micelle Detergent, and Nanodisc. These proteins can be utilized for BLI, ELISA, SPR, and Immunization, among other applications.

Product list

Source: ACROBiosystems Inc.