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|
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