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Description

The melanocortin-1 receptor (MC1) is a member of the G-protein-coupled receptor family of proteins that is responsible for regulating skin and hair color. The MC1 receptor is regulated by the physiological agonists alpha-melanocyte-stimulating hormone (alphaMSH) and adrenocorticotropic hormone (ACTH), and antagonist agouti signaling protein (ASP) (Rouzud et al., 2005). In 1995 a landmark study demonstrated that over 80% of humans with red hair or fair skin have a dysfunctional variant of the MC1 gene (Valverde et al., 1995). MC1 is, therefore, a major determinant of sun sensitivity and genetic risk factor for melanoma and non-melanoma skin cancer. Millipore&prime,s MC1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression, thus, they are ideal HTS tools for screening of agonists and antagonists of MC1. The membrane preparations exhibit a Kd of 1.3nM for [125I]-[Nle4, D-Phe7]-&alpha,-MSH (NDP-&alpha,MSH). With 0.3 nM [125I]-NDP-&alpha,MSH, 5&mu,g/well MC1 Membrane Prep typically yields greater than 50-fold signal-to-background ratio.