Transmembrane Receptors

7-Transmembrane receptors (7-TM receptors), also known as G-protein-coupled receptors, are the largest family of cell surface receptors in the human genome and are integral membrane proteins containing seven membrane-spanning helices. 7-TMs are coupled to intracellular heterotrimeric G proteins, and on ligand binding undergo a conformational change which is transmitted to the G protein.

7-TM receptors are activated by a wide variety of ligands such as nucleotides, peptides, amines, Ca2+ and photons, and are classed into 6 groups - Class A, rhodopsin-like, Class B, the secretin receptor family, Class C, metabotropic glutamate receptors, Class D, fungal mating pheromone receptors, Class E, cyclic AMP receptors and Class F, the frizzled/smoothened receptors.

Mutations in GPCR can cause acquired and inherited diseases such as retinitis pigmentosa, hypo- and hyperthyroidism, nephrogenic diabetes insipidus, fertility disorders, and cancer but due to their large number, widespread distribution and important roles in cell physiology and biochemistry, 7-TM’s have an important role in human medicine and are the target of around half of all modern medicinal drugs.

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