Expression of MC4R has been reported in brain. Unlike the other melanocortin receptors, MC4R is not expressed in adrenal cortex or in melanocytes. G-protein Coupled Receptors (GPCRs) comprise one of the largest families of signaling molecules with more than a thousand members currently predicted to exist. All GPCRs share a structural motif consisting of seven membrane-spanning helices, and exist in both active and inactive forms. An array of activating ligands participate in the conformation of GPCRs which leads to signaling via G-proteins and downstream effectors. Ongoing studies have also shown the vast series of reactions which participate in the negative regulation of GPCRs. This "turn-off" activity has tremendous implications for the physiological action of the cell, and continues to drive pharmacological research for new drug candidates. Two blockbuster drugs which have been developed as GPCR-targeted pharmaceuticals are Zyprexa (Eli Lilly) and Claritin (Schering-Plough) which have multi-billion dollar shares of the mental health and allergy markets, respectively.
MC4; MC4 receptor; MC4-R; Melanocortin receptor 4
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