ChemiSCREEN™ Membrane Preparation Recombinant Human MC₁ Melanocortin Receptor

ChemiSCREEN™ Membrane Preparation Recombinant Human MC₁ Melanocortin Receptor

Chemicon (Millipore)

200 units

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'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]-α-MSH (NDP-αMSH). With 0.3 nM [¹²⁵I]-NDP-αMSH, 5µg/well MC₁ Membrane Prep typically yields greater than 50-fold signal-to-background ratio.

Radioligand binding assay and GTPγS binding.

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This intronless gene encodes the receptor protein for melanocyte-stimulating hormone (MSH). The encoded protein, a seven pass transmembrane G protein coupled receptor, controls melanogenesis. Two types of melanin exist: red pheomelanin and black eumelanin. Gene mutations that lead to a loss in function are associated with increased pheomelanin production, which leads to lighter skin and hair color. Eumelanin is photoprotective but pheomelanin may contribute to UV-induced skin damage by generating free radicals upon UV radiation. Binding of MSH to its receptor activates the receptor and stimulates eumelanin synthesis. This receptor is a major determining factor in sun sensitivity and is a genetic risk factor for melanoma and non-melanoma skin cancer. Over 30 variant alleles have been identified which correlate with skin and hair color, providing evidence that this gene is an important component in determining normal human pigment variation.

FUNCTION: SwissProt: Q01726 # Receptor for MSH (alpha, beta and gamma) and ACTH. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
SIZE: 317 amino acids; 34706 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Melanocytes and corticoadrenal tissue.
SIMILARITY: SwissProt: Q01726 ## Belongs to the G-protein coupled receptor 1 family.

Human

Table 1. Signal:background and specific binding values obtained in a competition binding assay with MC₁ Receptor membrane prep.

	10 µg/well	5 µg/well
Signal:Background	133	146.6
Specific Binding (cpm)	31544	25485

B_max for [¹²⁵I]-NDP-αMSH binding: 13.7 pmol/mg protein
K_d for [¹²⁵I]-NDP-αMSH binding: ~1.3 nM

Chem-1

Chemicon

Chem-1

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membranes protein were adjusted to 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80°C.

MC1

Q01726

peptide

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Melanocortin

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A

• MC1R
• MSHR
• MGC14337
• MC1-R
• MSH-R

GPCR Membrane Preparations

ChemiSCREEN™ Membrane Preparation Recombinant Human MC₁ Melanocortin Receptor

NM_002386.2

GPCR