melanocortin receptor activity
Definition
Target type: molecularfunction
Combining with melanocortin to initiate a change in cell activity. [GOC:ai]
Melanocortin receptors are a family of G protein-coupled receptors (GPCRs) that are involved in a wide range of physiological processes, including pigmentation, energy homeostasis, stress response, and inflammation. They are activated by melanocortins, a group of peptides that include alpha-melanocyte-stimulating hormone (α-MSH), adrenocorticotropic hormone (ACTH), and β-endorphin. Upon binding of melanocortins, melanocortin receptors activate a signaling cascade that ultimately leads to the production of cyclic adenosine monophosphate (cAMP). cAMP then activates protein kinase A (PKA), which phosphorylates and activates downstream target proteins, leading to a variety of cellular responses.
Melanocortin receptors are expressed in a wide range of tissues, including the skin, brain, pituitary gland, adrenal glands, and immune cells. The specific functions of melanocortin receptors vary depending on the receptor subtype and the tissue in which they are expressed.
Melanocortin receptor 1 (MC1R) is primarily involved in pigmentation. Activation of MC1R by α-MSH leads to the production of melanin, a pigment that gives skin, hair, and eyes their color. MC1R mutations are associated with red hair and fair skin.
Melanocortin receptor 2 (MC2R) is expressed in the adrenal glands and is involved in the regulation of cortisol production. ACTH binds to MC2R and stimulates the synthesis and release of cortisol, a hormone that plays a role in stress response.
Melanocortin receptor 3 (MC3R) and melanocortin receptor 4 (MC4R) are expressed in the brain and are involved in the regulation of energy homeostasis. MC3R and MC4R mediate the anorexigenic effects of melanocortins, which suppress appetite and promote weight loss.
Melanocortin receptor 5 (MC5R) is expressed in the skin and other tissues and is involved in the regulation of inflammation. Activation of MC5R by α-MSH has anti-inflammatory effects.
Melanocortin receptors are important therapeutic targets for a variety of diseases, including obesity, skin disorders, and inflammation. Drugs that activate or block melanocortin receptors are currently being developed for these conditions.'
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Proteins (4)
| Protein | Definition | Taxonomy |
|---|---|---|
| Melanocortin receptor 5 | A melanocortin receptor 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P33032] | Homo sapiens (human) |
| Melanocyte-stimulating hormone receptor | A melanocyte-stimulating hormone receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q01726] | Homo sapiens (human) |
| Melanocortin receptor 3 | A melanocortin receptor 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41968] | Homo sapiens (human) |
| Melanocortin receptor 4 | A melanocortin receptor 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P32245] | Homo sapiens (human) |
Compounds (25)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| amiodarone | amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance. | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| astemizole | astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position. Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects. | benzimidazoles; piperidines | anti-allergic agent; anticoronaviral agent; H1-receptor antagonist |
| chlorpromazine | chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup. | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| ciglitazone | ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist. ciglitazone: structure given in second source; PPAR agonist used for type II diabetes | aromatic ether; thiazolidinone | antineoplastic agent; insulin-sensitizing drug |
| econazole | 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. Econazole: An imidazole derivative that is commonly used as a topical antifungal agent. | dichlorobenzene; ether; imidazoles; monochlorobenzenes | |
| fluphenazine | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug | |
| miconazole | 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes. Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion. | dichlorobenzene; ether; imidazoles | |
| dibenzothiazyl disulfide | dibenzothiazol-2-yl disulfide : An organic disulfide resulting from the formal oxidative coupling of the thiol groups of two molecules of 1,3-benzothiazole-2-thiol. It is used as an accelerator in the rubber industry. dibenzothiazyl disulfide: vulcanizing accelerant | benzothiazoles; organic disulfide | allergen |
| sterogenol | cetylpyridinium bromide : A pyridinium salt that has N-hexadecylpyridinium as the cation and bromide as the anion. hexadecylpyridinium bromide: structure in first source | bromide salt; pyridinium salt | antiseptic drug; EC 2.7.11.18 (myosin-light-chain kinase) inhibitor; surfactant |
| paclitaxel | Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| sertraline | sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder. Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression. | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| melanotan-ii | melanotan-II: synthetic cyclic heptapeptide, an analog of alpha-melanotropin (4,10); capable of stimulating melanin synthesis & promoting rapid tanning of skin; currently in trials for use in the prevention of sunlight-induced skin cancer | organic molecular entity | |
| tamoxifen | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator | |
| pmx 53 | |||
| ml 00253764 | 2-(2-(2-(5-bromo-2-methoxyphenyl)ethyl)-3-fluorophenyl)-4,5-dihydro-1H-imidazole: structure in first source | ||
| shu 9119 | SHU 9119: an agouti mimetic; structure in first source | ||
| bms-470539 | BMS-470539: a selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice; structure in first source | ||
| bremelanotide | bremelanotide: a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system; | oligopeptide | |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | |||
| acetyl-histidyl-phenylalanyl-arginyl-tryptophanamide | |||
| ac-his-dphe-arg-trp-nh2 | |||
| rm-493 | setmelanotide: an anti-obesity agent | ||
| alpha-msh | peptide hormone | anti-inflammatory agent | |
| msh, 4-nle-7-phe-alpha- | polypeptide | dermatologic drug | |
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source |