G protein-coupled receptors (GPCRs) are the largest family of membrane proteins. The primary function of GPCRs is to transduce a wide and diverse array of extracellular stimuli such as biogenic amines, peptides, hormones, neurotransmitters, ions, odorants, and photons into intracellular signals that regulate a myriad of physiological processes including cell metabolism, cell differentiation, growth, neurotransmission, and sensory perception. GPCRs have also been implicated in a large number of diseases, such as type 2 diabetes mellitus (T2DM), obesity, depression, cancer, Alzheimer’s disease, and many others. Therefore, GPCRs have become the most successful drug target class in drug target for the treatment of a variety of diseases.
The common molecular structure of GPCRs consists of seven transmembrane alpha helices, and these domains divide the receptor into extracellular N-terminus, intracellular C-terminus, three extracellular loops and three intracellular loops.
The extracellular ring contains two highly conserved cysteine residues, which can stabilize the spatial structure of the receptor by forming disulfide bonds. There is a G-protein binding site on the intracellular loop.
Schematic diagram of the classic GPCRs
It is extremely difficult to obtain biologically active soluble GPCRs antigen because of the limited extracellular exposure of GPCRs target, low cell surface expression, protein aggregation and other factors. The full-length structure to ensure the natural conformation of GPCRs antigen is of great significance to drug development. ACROBiosystems has specially built platform solutions of VLP, Micelle Detergent and Nanodisc to provide you with full-length GPCRs proteins including GPRC5D, CXCR4, CCR5, CCR8, which can be used for Immunization, ELISA, SPR, BLI etc.
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