Melanocortin receptors in GtoPdb v.2023.1
IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F38/2023.1
Melanocortin receptors in GtoPdb v.2023.1
Vanni Caruso1, Biao-Xin Chai2, Adrian J. L. Clark3, Roger D. Cone2, Alex N. Eberle4, Sadaf Farooqi5, Tung M.
Fong6, Ira Gantz7, Carrie Haskell-Luevano8, Victor J. Hruby9, Kathleen G. Mountjoy10, Colin Pouton11, Helgi
Schiöth12, Jeffrey B. Tatro13 and Jarl E. S. Wikberg12
1. University of Tasmania, Australia
2. University of Michigan, USA
3. St. Bartholomew's Hospital, UK
4. Universitsspital, Switzerland
5. University of Cambridge, UK
6. Vyluma Inc, USA
7. Merck & Co. Inc., USA
8. University of Minnesota, USA
9. University of Arizona, USA
10. University of Auckland, New Zealand
11. University of Bath, UK
12. Uppsala University, Sweden
13. New England Medical Center Hospital, USA
Abstract
Melanocortin receptors (provisional nomenclature as recommended by NC-IUPHAR [41]) are activated by
members of the melanocortin family (α-MSH, β-MSH and γ-MSH forms; δ form is not found in mammals)
and adrenocorticotrophin (ACTH). Endogenous antagonists include agouti and agouti-related protein.
ACTH(1-24) was approved by the US FDA as a diagnostic agent for adrenal function test. setmelanotide was
approved by the US FDA for weight management in patients with POMC, PCSK1 or LEPR defiency,
bremelanotide was approved by the US FDA for generalized hypoactive sexual desire disorder in
premenopausal women, and NDP-MSH (afamelanotide) was approved by the EMA for the treatment of
erythropoietic protoporphyria. Several synthetic melanocortin receptor agonists are under clinical
development.
Contents
This is a citation summary for Melanocortin receptors in the Guide to Pharmacology database (GtoPdb). It
exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database
by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which
are given here under database links.
GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a
reference work which is most usefully represented as an on-line database. As in any publication this work
should be appropriately cited, and the papers it cites should also be recognized. This document provides a
citation for the relevant parts of the database, and also provides a reference list for the research cited by
those parts. For further details see [11].
Please note that the database version for the citations given in GtoPdb are to the most recent preceding
version in which the family or its subfamilies and targets were substantially changed. The links below are to
the current version. If you need to consult the cited version, rather than the most recent version, please
contact the GtoPdb curators.
Database links
Melanocortin receptors
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=38
Introduction to Melanocortin receptors
https://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=38
Receptors
MC1 receptor
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=282
MC2 receptor
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=283
MC3 receptor
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=284
MC4 receptor
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=285
MC5 receptor
https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=286
References
1. Adan RA, Szklarczyk AW, Oosterom J, Brakkee JH, Nijenhuis WA, Schaaper WM, Meloen RH and Gispen
WH. (1999) Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors
and on grooming behavior in the rat. Eur J Pharmacol 378: 249-258 [PMID:10493100]
2. Al-Obeidi F, Hruby VJ, Castrucci AM and Hadley ME. (1989) Design of potent linear α-melanotropin 4-10
analogues modified in positions 5 and 10. J Med Chem 32: 174-179 [PMID:2535874]
3. Argiolas A and Melis MR. (2013) Neuropeptides and central control of sexual behaviour from the past to
the present: a review. Prog Neurobiol 108: 80-107 [PMID:23851261]
4. Balse-Srinivasan P, Grieco P, Cai M, Trivedi D and Hruby VJ. (2003) Structure-activity relationships of
novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the
human MC3R and human MC5R. J Med Chem 46: 3728-33 [PMID:12904077]
5. Bednarek MA, MacNeil T, Kalyani RN, Tang R, Van der Ploeg LH and Weinberg DH. (2001) Selective,
high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their
synthesis and biological evaluation in vitro. J Med Chem 44: 3665-72 [PMID:11606131]
6. Benoit SC, Schwartz MW, Lachey JL, Hagan MM, Rushing PA, Blake KA, Yagaloff KA, Kurylko G, Franco
L and Danhoo W et al.. (2000) A novel selective melanocortin-4 receptor agonist reduces food intake in
rats and mice without producing aversive consequences. J Neurosci 20: 3442-8 [PMID:10777807]
7. Bertolini A, Tacchi R and Vergoni AV. (2009) Brain effects of melanocortins. Pharmacol Res 59: 13-47
[PMID:18996199]
8. Boman A, Jonassen TEN and Lundstedt T. (2007) Phenyl pyrrole aminoguanidine derivatives Patent
number: WO2007141343A1. Assignee: Action Pharma A/S. Priority date: 09/06/2006. Publication date:
13/12/2007.
9. Borowsky B, Durkin MM, Ogozalek K, Marzabadi MR, DeLeon J, Lagu B, Heurich R, Lichtblau H,
Shaposhnik Z, Daniewska I, Blackburn TP, Branchek TA, Gerald C, Vaysse PJ and Forray C. (2002)
Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor
antagonist. Nat Med 8: 825-830 [PMID:12118247]
10. Boston BA and Cone RD. (1996) Characterization of melanocortin receptor subtype expression in
murine adipose tissues and in the 3T3-L1 cell line. Endocrinology 137: 2043-50 [PMID:8612546]
11. Buneman P, Christie G, Davies JA, Dimitrellou R, Harding SD, Pawson AJ, Sharman JL and Wu Y. (2020)
Why data citation isn't working, and what to do about it Database 2020 [PMID:32367113]
12. Butler AA, Kesterson RA, Khong K, Cullen MJ, Pelleymounter MA, Dekoning J, Baetscher M and Cone RD.
(2000) A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse.
Endocrinology 141: 3518-21 [PMID:10965927]
13. Böhm M, Eickelmann M, Li Z, Schneider SW, Oji V, Diederichs S, Barsh GS, Vogt A, Stieler K and BlumePeytavi U et al.. (2005) Detection of functionally active melanocortin receptors and evidence for an
immunoregulatory activity of alpha-melanocyte-stimulating hormone in human dermal papilla cells.
Endocrinology 146: 4635-46 [PMID:16081629]
14. Carla Caruso, L. C., Daniela Durand and Teresa N. Scimonelli and Mercedes Lasaga. (2012)
Melanocortins: Anti-Inflammatory and Neuroprotective Peptides In Neurodegeneration Edited by L.
Miguel Martins: InTech:
15. Caruso V, Lagerström MC, Olszewski PK, Fredriksson R and Schiöth HB. (2014) Synaptic changes
induced by melanocortin signalling. Nat Rev N (...truncated)
