Melanocortin Receptor
Melanocortins, primarily consisting of a-melanocyte stimulating hormone (MSH), bMSH, g-MSH, and adrenocorticotropin (ACTH), are small peptide hormones derived from tissue-specific post-translational processing of a pre-prohormone, proopiomelanocortin(POMC). Functions of melanocortins on pigmentation and adrenal steroidogenesis are mediated by cell surface receptors that are coupled to the stimulatory heterotrimeric G protein, Gs. With the cloning of the classical MSH receptor and ACTH receptor, it was soon realized that three additional G protein-coupled receptors (GPCRs) with significant homology to the MSH receptor and ACTH receptor exist in mammalian genomes. The five cell-surface GPCRs that mediate melanocortin action are named MC1R (MSH receptor), MC2R (ACTH receptor), MC3R to MC5R, based on the sequence of their cloning. All five MCRs are coupled to the stimulatory G protein, increasing intracellular cAMP levels when the receptors are activated. MCRs also activate other signaling pathways, especially MAPKs, as shown extensively in other GPCRs. When the signaling in the canonical Gs-cAMP and non-canonical pathways are compared, differential response is observed in some instances. For example, the endogenous antagonist AgRP, while decreasing cAMP generation, stimulates ERK1/2 phosphorylation, therefore serving as agonist in the ERK1/2 pathway in both MC3R and MC4R.
References
1.Tao YX. Biochim Biophys Acta Mol Basis Dis. 2017;1863(10 Pt A):2411–2413.
References
1.Tao YX. Biochim Biophys Acta Mol Basis Dis. 2017;1863(10 Pt A):2411–2413.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(14)
Dopamine Receptor(181)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(15)
Urotensin Receptor(4)
Vasopressin Receptor(20)
Melanocortin Receptor
-
ACTH 11-24 acetate(4237-93-8 free base)
catalog no : M37912
cas no: 79190-56-0
ACTH 11-24 acetate(4237-93-8 free base) (Adrenocorticotropic Hormone (11-24) acetate) is a fragment of adrenocorticotrophin, induces cortisol release. -
PF-07258669
catalog no : M36282
cas no: 2755890-53-8
PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite. -
Dersimelagon
catalog no : M34067
cas no: 1835256-48-8
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values ??of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. -
Setmelanotide Acetate(920014-72-8 free base)
catalog no : M33122
cas no: 2759937-80-7
Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively). -
BMS-470539 dihydrochloride
catalog no : M32812
cas no: 2341796-82-3
BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity.