Molecular cloning, expression, and characterization of a fifth melanocortin receptor.

摘要: Abstract We report the isolation of a gene encoding novel member family melanocortin receptors. The mouse melanocortin-5 receptor (mMC5R) responds to melanocortins with an increase in intracellular cyclic 3′, 5′-adenosine monophosphate (cAMP) concentrations. Stimulation mMC5R by revealed hierarchy potency which α-melanocyte stimulating hormone (α-MSH) > β-melanocyte (β-MSH) adrenocorticotropic (ACTH) γ-melanocyte (γ-MSH). Further structure-activity studies indicated that amino- and carboxyl-terminal portions α-MSH appear be key determinants activation whereas core heptapeptide sequence is devoid pharmacological activity. Northern blot analysis demonstrated expression mRNA skeletal muscle, lung, spleen, brain.