New Insights into G-Protein-Coupled Receptor Signaling from the Melanocortin Receptor System

Rana, Brinda K.

doi:10.1124/mol.64.1.1

Cited by 11 publications

(4 citation statements)

References 31 publications

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“…All are functionally coupled to adenylyl cyclase and mediate their effects primarily by activating a cAMP-dependent signaling pathway. MCRs share many features with other G protein-coupled receptors (Rana, 2003): they have several potential N-glycosylation sites in their amino-terminal domains, consensus recognition sites for protein kinase C and/or A (PKA), and conserved cysteines in their carboxyl termini Abdel-Malek, 2001). Ligand affinity, tissue distribution, and functions of each receptor subtype are reported in Table 1.…”

Section: Melanocortin Receptors and Their Endogenous Antagonistsmentioning

confidence: 99%

Targeting Melanocortin Receptors as a Novel Strategy to Control Inflammation

et al. 2004

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Section: Melanocortin Receptors and Their Endogenous Antagonistsmentioning

confidence: 99%

Targeting Melanocortin Receptors as a Novel Strategy to Control Inflammation

et al. 2004

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“…These compounds are known as “inverse agonists”, given they have the opposite effect of agonists . Because the inverse agonists may have preferred therapeutic applications, − generation of the constitutively active mutants of GPCRs is a useful strategy to develop these compounds. Dupre et al reported that in human CysLT 1 , the substitution of Ile232 in the third intracellular loop to Arg (I232R) and of Asp106 in the TM2 to Ala (N106A) stabilizes the active form and leads to a significant increase in the basal production of inositol phosphates (IPs), demonstrating the construction of constitutively active mutants of human CysLT 1 .…”

Section: Cys-lt Receptorsmentioning

confidence: 99%

Leukotriene Receptors

Nakamura

Shimizu

2011

Chem. Rev.

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“…MC3R and MC4R are found in the central nervous system but are notably absent from melanocytes [84]; both are highly expressed in the hypothalamus, where they are involved in energy homeostasis. ACTHR is expressed in the adrenal cortex and MC5R in peripheral cells such as adipocytes [85].…”

Section: The Melanocortin Receptorsmentioning

confidence: 99%

MC1R and the response of melanocytes to ultraviolet radiation

Rouzaud

Kadekaro

Abdel‐Malek

et al. 2005

Mutation Research/Fundamental and Molecular Mechanisms of Mutag

145

102

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The constitutive color of our skin plays a dramatic role in our photoprotection from solar ultraviolet radiation (UVR) that reaches the Earth and in minimizing DNA damage that gives rise to skin cancer. More than 120 genes have been identified and shown to regulate pigmentation, one of the key genes being melanocortin 1 receptor (MC1R) that encodes the melanocortin 1 receptor (MC1R), a seven-transmembrane G protein-coupled receptor expressed on the surface of melanocytes. Modulation of MC1R function regulates melanin synthesis by melanocytes qualitatively and quantitatively. The MC1R is regulated by the physiological agonists alpha-melanocyte-stimulating hormone (alphaMSH) and adrenocorticotropic hormone (ACTH), and antagonist agouti signaling protein (ASP). Activation of the MC1R by binding of an agonist stimulates the synthesis of eumelanin primarily via activation of adenylate cyclase. The significance of cutaneous pigmentation lies in the photoprotective effect of melanin, particularly eumelanin, against sun-induced carcinogenesis. Epidermal melanocytes and keratinocytes respond to UVR by increasing their expression of alphaMSH and ACTH, which up-regulate the expression of MC1R, and consequently enhance the response of melanocytes to melanocortins. Constitutive skin pigmentation dramatically affects the incidence of skin cancer. The pigmentary phenotype characterized by red hair, fair complexion, inability to tan and tendency to freckle is an independent risk factor for all skin cancers, including melanoma. The MC1R gene is highly polymorphic in human populations, and allelic variation at this locus accounts, to a large extent, for the variation in pigmentary phenotypes and skin phototypes (SPT) in humans. Several allelic variants of the MC1R gene are associated with the red hair and fair skin (RHC) phenotype, and carrying one of these variants is thought to diminish the ability of the epidermis to respond to DNA damage elicited by UVR. The MC1R gene is considered a melanoma susceptibility gene, and its significance in determining the risk for skin cancer is of tremendous interest.

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New Insights into G-Protein-Coupled Receptor Signaling from the Melanocortin Receptor System

Cited by 11 publications

References 31 publications

Targeting Melanocortin Receptors as a Novel Strategy to Control Inflammation

Targeting Melanocortin Receptors as a Novel Strategy to Control Inflammation

Leukotriene Receptors

MC1R and the response of melanocytes to ultraviolet radiation

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