G-Protein Coupled Receptor Family

G protein-coupled receptors (GPCRs) constitute a large protein family of receptors which detect extracellular molecules and activate internal signal transduction pathways that ultimately activate cellular responses. GPCRs are coupled with G proteins and pass through the cell membrane seven times, thus they are called seven-transmembrane receptors. GPCRs are found only in eukaryotes, including animals, yeast, and choanoflagellates.

Fig.1 G-protein-coupled receptor (GPCR) signaling in platelets. (Gurbel, 2015)

As an important drug target, about 34% of all FDA approved drugs target the GPCRs family. The sales volume for this type of drugs is estimated to be 180 billion US Dollars. GPCRs constitute several membrane proteins that are activated by hormones and neurotransmitters to trigger cellular signaling pathways and are involved in many diseases. To date, most drugs have targeted the class A (rhodopsin-like family). The Class B (secretin-like family) has been targeted for the treatment of metabolic diseases such as diabetes mellitus, as well as cardiovascular diseases, bone disorders, neurodegeneration, malignancies, and neuropsychiatric disorders.

Nearly 800 different human genes, about 4% of the entire protein-coding genome, have been predicted to code for them from genome sequence analysis. G-protein–coupled receptor is classically divided into three main classes, Class A (Rhodopsin-like), Class B (Secretin-like), Class C (Glutamate Receptor-like) and others (Adhesion, Frizzled, Taste type-2, unclassified). There is no detectable shared sequence homology between these classes. Here shows part of GPCRs in humans:

Human G-Protein Coupled Receptor Members
GPR1	GPR101	GPR119	GPR12	GPR132	GPR135	GPR139	GPR142
GPR143	GPR146	GPR148	GPR149	GPR15	GPR150	GPR151	GPR152
GPR153	GPR156	GPR157	GPR158	GPR160	GPR161	GPR162	GPR17
GPR171	GPR173	GPR174	GPR176	GPR179	GPR18	GPR182	GPR183
GPR19	GPR20	GPR21	GPR22	GPR25	GPR26	GPR27	GPR3
GPR31	GPR32	GPR84	GPR33	GPR34	GPR35	GPR37	GPR37L1
GPR39	GPR4	GPR85	GPR87	GPR50	GPR52	GPR55	GPR6
GPR61	GPR62	GPR88	GPR65	GPR68	GPR75	GPR78	GPR98
GPR83

Aided by cutting-edge Magic™ membrane protein production platform, Creative Biolabs is proud to offer the preparation of these targets in required formats using various strategies, such as detergent micelles, proteoliposomes, nanodiscs, lipoparticles, polymers, stable cell line.

Magic™ membrane protein production platform – Creative Biolabs

Meanwhile, our Magic™ membrane protein antibody discovery platform can help to discover antibodies against these targets, even fully humanized antibodies, by various approaches including hybridoma technology, phage display technology, etc. We also present DNA immunization service for anti-membrane protein antibody development. Please feel free to contact us for more information.

Reference

Gurbel PA, et al. (2015). G-protein-coupled receptors signaling pathways in new antiplatelet drug development. Arterioscler Thromb Vasc Biol. 35(3): 500-12.

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