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MC1 receptor

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Target not currently curated in GtoImmuPdb

Target id: 282

Nomenclature: MC1 receptor

Family: Melanocortin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 317 16q24.3 MC1R melanocortin 1 receptor 26
Mouse 7 315 8 72.1 cM Mc1r melanocortin 1 receptor 26
Rat 7 325 19q12 Mc1r melanocortin 1 receptor
Previous and Unofficial Names Click here for help
MSH-R | melanocortin 1 receptor (alpha melanocyte stimulating hormone receptor)
Database Links Click here for help
Specialist databases
GPCRdb mshr_human (Hs), mshr_mouse (Mm)
Other databases
Alphafold Q01726 (Hs), Q01727 (Mm)
ChEMBL Target CHEMBL3795 (Hs), CHEMBL4077 (Mm)
Ensembl Gene ENSG00000258839 (Hs), ENSMUSG00000074037 (Mm), ENSRNOG00000038193 (Rn)
Entrez Gene 4157 (Hs), 17199 (Mm), 292083 (Rn)
Human Protein Atlas ENSG00000258839 (Hs)
KEGG Gene hsa:4157 (Hs), mmu:17199 (Mm), rno:292083 (Rn)
OMIM 155555 (Hs)
Orphanet ORPHA139778 (Hs)
Pharos Q01726 (Hs)
RefSeq Nucleotide NM_002386 (Hs), NM_008559 (Mm)
RefSeq Protein NP_002377 (Hs), NP_032585 (Mm)
UniProtKB Q01726 (Hs), Q01727 (Mm)
Wikipedia MC1R (Hs)
Associated Proteins Click here for help
Interacting Proteins
Name Effect References
Opsin 3 Opsin 3 (OPN3 or Encephalopsin) functional and physical association, negatively modulates melanin producing signals in epidermal melanocytes through Gi protein alpha subunit (Gαi) 27
Natural/Endogenous Ligands Click here for help
ACTH {Sp: Human} , ACTH {Sp: Mouse, Rat}
agouti {Sp: Mouse}
β-MSH {Sp: Human}
α-MSH {Sp: Human, Mouse, Rat}
γ-MSH {Sp: Human, Mouse, Rat}
β-MSH {Sp: Mouse} , β-MSH {Sp: Rat}
Comments: α-MSH is the principal endogenous agonist. Endogenous antagonists are agouti and agouti-related protein. For representations of the rodent orthologues of these peptides see agouti (mouse), agouti (rat) and agouti-related protein (mouse).
Potency order of endogenous agonists (Human)
α-MSH (POMC, P01189) > β-MSH (POMC, P01189) > ACTH (POMC, P01189), γ-MSH (POMC, P01189)

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]NDP-MSH Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.5 pKd 20
⤷ pKd 9.5 (Kd 3.3x10-10 M) [20]
SHU9119 Peptide Click here for species-specific activity table Hs Partial agonist 9.2 pKd 14,30
⤷ pKd 9.2 [14,30]
MS05 Peptide Hs Full agonist 9.1 pKd 33
⤷ pKd 9.1 [33]
HS014 Peptide Click here for species-specific activity table Hs Partial agonist 7.0 pKd 30
⤷ pKd 7.0 [30]
ACTH {Sp: Human} Peptide Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Agonist 8.6 pKi 29
⤷ pKi 8.6 (Ki 2.5x10-9 M) [29]
setmelanotide Peptide Approved drug Click here for species-specific activity table Hs Agonist 8.4 pKi 21
⤷ pKi 8.4 (Ki 3.9x10-9 M) [21]
bremelanotide Peptide Approved drug Click here for species-specific activity table Hs Agonist 8.2 pKi 10
⤷ pKi 8.2 (Ki 6.4x10-9 M) [10]
Description: Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC1 receptor.
afamelanotide Peptide Approved drug Click here for species-specific activity table Hs Full agonist 10.0 pIC50 23,31
⤷ pIC50 10.0 [23,31]
MT-II Peptide Click here for species-specific activity table Hs Full agonist 9.4 pIC50 1,23
⤷ pIC50 9.4 [1,23]
α-MSH {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.4 pIC50 23
⤷ pIC50 8.4 [23]
Agonist Comments
The human MC1 compared to the mouse MC1 is "supersensitive" to the melanocortin peptides [24].

A selective MC1 receptor agonist with nanomolar potency has recently been described [13]. cAMP but no binding data were published.

Ro27-3225 is a selective MC1R and MC4R agonist [2]. cAMP but no binding data were published.

[125I]NDP-MSH, [125I]MT-II, [125I]SHU9119, [125I]Nle7-α-MSH are common radioligands used to study MC1, 3, 4 and MC5.
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
agouti {Sp: Mouse} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Inverse agonist 8.6 pKd 19,22
⤷ pKd 8.6 [19,22]
HS024 Peptide Click here for species-specific activity table Hs Antagonist 7.7 pKd 18
⤷ pKd 7.7 [18]
ASIP [90-132 (L89Y)] Peptide Click here for species-specific activity table Hs Inverse agonist 8.1 pIC50 36-37
⤷ pIC50 8.1 [36-37]
View species-specific antagonist tables
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  24
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
G protein (identity unknown) Other - See Comments
Comments:  Melanocortin activation of the murine MC1R mobilizes intracellular calcium via an incompletely understood pathway.
Alternative rescue transduction mechanism: (transducer unknown, effector/response protein kinase B (Akt)). This pathway is only activated when there is insufficient production of cAMP due to loss of function mutations and is currently associated with only the protective activity against cancer.
References:  5,25
Tissue Distribution Click here for help
Endothelial cells.
Species:  Human
Technique:  RT-PCR
References:  12
Melanoma cells.
Species:  Human
Technique:  PCR and Northern Blotting.
References:  9
Neutrophils.
Species:  Human
Technique:  RT-PCR
References:  7
Dermal papilla cells.
Species:  Human
Technique:  RT-PCR and immunofluorescence.
References:  4
Pituitary and testes.
Species:  Human
Technique:  PCR and hybridisation.
References:  8
Macrophages.
Species:  Mouse
Technique:  RT-PCR
References:  32
Fibroblasts.
Species:  Mouse
Technique:  RT-PCR and Northern Blotting.
References:  3
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of intracellular cAMP levels.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in cAMP levels.
References:  36
Measurement of cAMP in cell lines transfected with the MC1 receptor.
Species:  Human
Tissue:  HEK 293 and COS cells.
Response measured:  Intracellular cAMP accumulation.
References:  24
Measurement of intracellular Ca2+ levels in HEK 293 cells transfected with the MC1 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Mobilization of [Ca2+]i.
References:  25
Xenopus melanophore pigment dispersion assay.
Species:  Human
Tissue:  Xenopus melanophores transfected with human MC1.
Response measured:  Melanophore aggregation and dispersion measured by optical density.
References:  15
Physiological Functions Click here for help
In mammals the MC1 expressed by the dermal melanocyte regulates the synthesis of eumelanin (black-brown pigment) versus phaeomelanin (yellow-red pigment). α-MSH acts at the melanocyte MC1 to elevate enzymes like tyrosinase, which are necessary for eumelanin synthesis, replacing synthesis of the default yellow-red phaeolmelanin pigments.
Species:  Mouse
Tissue:  Skin
References:  11
MC1 expressed by leukocytes may be responsible for some of the anti-inflammatory actions of α-MSH.
Species:  Human
Tissue:  Not Specified
References:  35
Stimulation of human dermal microvascular endothelial cells (HDMECs) with α-MSH causes an increase in expression of interleukin-8 (IL-8). This may have a role in the anti-inflammatory actions of α-MSH.
Species:  Human
Tissue:  HDMEC cells.
References:  12
Anti-cancer protective functions independent from pigmentation. Human MC1R can Initiate DNA repair protocols in response to carcinogenic mutations and prevent oxidative damage through induction of antioxidant enzymes (catalase, superoxide dismutase (SOD1)).
Species:  Human
Tissue:  Melanocytes
References:  16-17
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Mc1rE-tob Mc1rE-tob/Mc1rE-tob
M. m. domesticus poschiavinus		 MGI:99456  MP:0002075 abnormal coat/hair pigmentation
Mc1rtaw Mc1rtaw/Mc1rtaw
M. m. molossinus		 MGI:99456  MP:0002075 abnormal coat/hair pigmentation PMID: 15653560 
Mc1rtaw Mc1rtaw/Mc1rtaw
M. m. molossinus		 MGI:99456  MP:0000015 abnormal ear pigmentation PMID: 15653560 
Mc1re Mc1re/Mc1re
C57BL/6Ha		 MGI:99456  MP:0004382 abnormal hair follicle melanogenesis PMID: 1098946 
Mc1re Mc1re/Mc1re
C57BL/6J-Mc1r/J		 MGI:99456  MP:0001224 abnormal keratinocyte apoptosis PMID: 16988713 
Mc1re Mc1re/Mc1re
C57BL/6J-Mc1r/J		 MGI:99456  MP:0005077 abnormal melanogenesis PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk Mc1re/Mc1re,Tg(KRT14-Kitl)1Takk/0
involves: C57BL/6 * SJL		 MGI:3607789  MGI:99456  MP:0005077 abnormal melanogenesis PMID: 16988713 
Mc1re-J Mc1re-J/Mc1re-J
B6.C-H2-Ab1/KhEg-Mc1r/J		 MGI:99456  MP:0001970 abnormal pain threshold PMID: 15277941 
Mc1re Mc1re/Mc1re
C57BL/6		 MGI:99456  MP:0001970 abnormal pain threshold PMID: 15994880 
Mc1re Mc1re/Mc1re
involves: C57BL/6Ha		 MGI:99456  MP:0006370 abnormal phaeomelanin content PMID: 17652101 
A|Mc1re|Pomctm1Sora|Tg(MC1R)1Jkn a/A,Mc1re/Mc1re,Pomctm1Sora/Pomctm1Sora,Tg(MC1R)1Jkn/?
involves: 129S6/SvEvTac * C57BL/6Ha		 MGI:3805879  MGI:87853  MGI:97742  MGI:99456  MP:0006370 abnormal phaeomelanin content PMID: 17652101 
a|Mc1re|Pomctm1Sora|Tg(MC1R)1Jkn a/a,Mc1re/Mc1re,Pomctm1Sora/Pomctm1Sora,Tg(MC1R)1Jkn/?
involves: 129S6/SvEvTac * C57BL/6Ha		 MGI:3805879  MGI:87853  MGI:97742  MGI:99456  MP:0006370 abnormal phaeomelanin content PMID: 17652101 
Mc1re Mc1re/Mc1re
C57BL/6J-Mc1r/J		 MGI:99456  MP:0002095 abnormal skin pigmentation PMID: 16988713 
Mc1rtaw Mc1rtaw/Mc1rtaw
M. m. molossinus		 MGI:99456  MP:0002095 abnormal skin pigmentation PMID: 15653560 
Mc1rE-so Mc1rE-so/Mc1rE-so
C3H		 MGI:99456  MP:0002095 abnormal skin pigmentation
Mc1r+|Mc1rE-so Mc1rE-so/Mc1r+
C3H		 MGI:99456  MP:0002095 abnormal skin pigmentation
Mc1rtaw Mc1rtaw/Mc1rtaw
M. m. molossinus		 MGI:99456  MP:0005174 abnormal tail pigmentation PMID: 15653560 
Mc1re Mc1re/Mc1re
C57BL/6		 MGI:99456  MP:0001968 abnormal touch/ nociception PMID: 15994880 
Mc1re Mc1re/Mc1re
C57BL/6		 MGI:99456  MP:0004270 analgesia PMID: 15994880 
Adamts20bt|Mc1re Adamts20bt/Adamts20bt,Mc1re/Mc1re
involves: C57BL/6Ha * DBA		 MGI:2660628  MGI:99456  MP:0002671 belted PMID: 5713933 
Mc1rE-tob Mc1rE-tob/Mc1rE-tob
M. m. domesticus poschiavinus		 MGI:99456  MP:0005409 darkened coat color
Mc1rE-so Mc1rE-so/Mc1rE-so
C3H		 MGI:99456  MP:0005409 darkened coat color
Mc1r+|Mc1rE-so Mc1rE-so/Mc1r+
C3H		 MGI:99456  MP:0005409 darkened coat color
Mc1re|Mlphln Mc1re/Mc1re,Mlphln/Mlphln
Not Specified		 MGI:2176380  MGI:99456  MP:0000371 diluted coat color PMID: 5713933 
Mc1rE-so Mc1rE-so/Mc1rE-so
C3H		 MGI:99456  MP:0001188 hyperpigmentation
Mc1r+|Mc1rE-so Mc1rE-so/Mc1r+
C3H		 MGI:99456  MP:0001188 hyperpigmentation
Mc1re Mc1re/Mc1re
C57BL/6J-Mc1r/J		 MGI:99456  MP:0004227 increased cellular sensitivity to ionizing radiation PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk|Xpctm1Brd Mc1re/Mc1re,Xpctm1Brd/Xpctm1Brd,Tg(KRT14-Kitl)1Takk/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL		 MGI:103557  MGI:3607789  MGI:99456  MP:0002020 increased tumor incidence PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk|Xpctm1Brd Mc1re/Mc1re,Xpctm1Brd/Xpctm1Brd,Tg(KRT14-Kitl)1Takk/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL		 MGI:103557  MGI:3607789  MGI:99456  MP:0001212 skin lesions PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk|Xpctm1Brd Mc1re/Mc1re,Xpctm1Brd/Xpctm1Brd,Tg(KRT14-Kitl)1Takk/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL		 MGI:103557  MGI:3607789  MGI:99456  MP:0004207 squamous cell carcinoma PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk|Xpctm1Brd Mc1re/Mc1re,Xpctm1Brd/Xpctm1Brd,Tg(KRT14-Kitl)1Takk/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL		 MGI:103557  MGI:3607789  MGI:99456  MP:0001219 thickened epidermis PMID: 16988713 
Mc1re|Tg(KRT14-Kitl)1Takk|Xpctm1Brd Mc1re/Mc1re,Xpctm1Brd/Xpctm1Brd,Tg(KRT14-Kitl)1Takk/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL		 MGI:103557  MGI:3607789  MGI:99456  MP:0001263 weight loss PMID: 16988713 
Ednrbs|Mc1re Ednrbs/Ednrbs,Mc1re/Mc1re
Not Specified		 MGI:102720  MGI:99456  MP:0002938 white spotting PMID: 5713933 
Mc1re Mc1re/Mc1re
C57BL/6Ha		 MGI:99456  MP:0003136 yellow coat color PMID: 5713933  767180 
Ednrbs|Mc1re Ednrbs/Ednrbs,Mc1re/Mc1re
Not Specified		 MGI:102720  MGI:99456  MP:0003136 yellow coat color PMID: 5713933 
Adamts20bt|Mc1re Adamts20bt/Adamts20bt,Mc1re/Mc1re
involves: C57BL/6Ha * DBA		 MGI:2660628  MGI:99456  MP:0003136 yellow coat color PMID: 5713933 
Mc1rtaw Mc1rtaw/Mc1rtaw
M. m. molossinus		 MGI:99456  MP:0003136 yellow coat color PMID: 15653560 
Mc1re|Mc1rtaw Mc1rtaw/Mc1re
involves: M. m. molossinus * C57BL/6J		 MGI:99456  MP:0003136 yellow coat color PMID: 10374067 
Mc1re Mc1re/Mc1re
involves: C57BL/6Ha		 MGI:99456  MP:0003136 yellow coat color PMID: 17652101 
A|Ay-Jkn|Mc1re Ay-Jkn/A,Mc1re/Mc1re
involves: C57BL/6Ha * C57BL/6N		 MGI:87853  MGI:99456  MP:0003136 yellow coat color PMID: 17652101 
A|Ay-Jkn|Mc1re|Tg(MC1R)1Jkn Ay-Jkn/A,Mc1re/Mc1re,Tg(MC1R)1Jkn/0
involves: C57BL/6Ha * C57BL/6N		 MGI:3805879  MGI:87853  MGI:99456  MP:0003136 yellow coat color PMID: 17652101 
A|Mc1re|Pomctm1Sora|Tg(MC1R)1Jkn a/A,Mc1re/Mc1re,Pomctm1Sora/Pomctm1Sora,Tg(MC1R)1Jkn/?
involves: 129S6/SvEvTac * C57BL/6Ha		 MGI:3805879  MGI:87853  MGI:97742  MGI:99456  MP:0003136 yellow coat color PMID: 17652101 
a|Mc1re|Pomctm1Sora|Tg(MC1R)1Jkn a/a,Mc1re/Mc1re,Pomctm1Sora/Pomctm1Sora,Tg(MC1R)1Jkn/?
involves: 129S6/SvEvTac * C57BL/6Ha		 MGI:3805879  MGI:87853  MGI:97742  MGI:99456  MP:0003136 yellow coat color PMID: 17652101 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Increased analgesia from kappa-opioid receptor agonist, female-specific
OMIM: 613098
Disease:  Large congenital melanocytic nevus
Synonyms: Congenital melanocytic nevus [Disease Ontology: DOID:3157]
Disease Ontology: DOID:3157
Orphanet: ORPHA626
Disease:  Melanoma, cutaneous malignant, susceptibility to, 5; CMM5
Synonyms: Familial melanoma [Orphanet: ORPHA618]
OMIM: 613099
Orphanet: ORPHA618
Disease:  Oculocutaneous albinism type 2
Synonyms: Oculocutaneous albinism [Disease Ontology: DOID:0050632]
Disease Ontology: DOID:0050632
OMIM: 203200
Orphanet: ORPHA79432
Disease:  Skin/hair/eye pigmentation, variation in, 2; SHEP2
OMIM: 266300
Role:  Increased susceptibility to UV-induced skin damage associated with variants in the MC1R gene.
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Human
Description:  There is a splice variant of the MC1 receptor termed MC1B, which has an additional 65 amino acids at the predicted intracellular, C-terminal tail. Pharmacologically this splice variant appears to be similar to the MC1 receptor.
References:  34
Type:  Naturally occurring mutations
Species:  Mouse
Description:  The MC1 maps to the extension locus, which was identified by classical geneticists to be one of the major determinants of mammalian coat color. Point mutations of the MC1 that alter its function are responsible for pigmentation phenotypes such as the red fox or yellow mouse.
References:  28
Biologically Significant Variant Comments
Common variations (polymorphisms) in the MC1R gene are associated with normal differences in skin and hair color. The MC1 receptor regulates the balance between eumelanin (associated with black hair and dark skin that tans easily) and pheomelanin (associated with fair hair, and easily burnt skin on UV exposure) production by melanocytes. MC1 receptor activation favours the production of eumelanin, whereas inactivating variants lead to pheomelanin production. Inactivating receptor polymorphisms are most common in people with red hair, fair skin, freckles, and an increased sensitivity to sun exposure. Inactivating mutations are also associated with increased risk of developing skin cancers, since the inability to produce sufficient eumelanin leaves fair skin more vulnerable to damage from sun exposure.
General Comments
Bioassays based on frog and lizard skin are also used. [6]

References

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1. Al-Obeidi F, Hruby VJ, Castrucci AM, 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]

2. Benoit SC, Schwartz MW, Lachey JL, Hagan MM, Rushing PA, Blake KA, Yagaloff KA, Kurylko G, Franco L, 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 (9): 3442-8. [PMID:10777807]

3. Boston BA, Cone RD. (1996) Characterization of melanocortin receptor subtype expression in murine adipose tissues and in the 3T3-L1 cell line. Endocrinology, 137 (5): 2043-50. [PMID:8612546]

4. Böhm M, Eickelmann M, Li Z, Schneider SW, Oji V, Diederichs S, Barsh GS, Vogt A, Stieler K, Blume-Peytavi 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 (11): 4635-46. [PMID:16081629]

5. Castejón-Griñán M, Herraiz C, Olivares C, Jiménez-Cervantes C, García-Borrón JC. (2018) cAMP-independent non-pigmentary actions of variant melanocortin 1 receptor: AKT-mediated activation of protective responses to oxidative DNA damage. Oncogene, 37 (27): 3631-3646. [PMID:29622793]

6. Castrucci AM, Hadley ME, Hruby VJ. (1984) Melanotropin bioassays: in vitro and in vivo comparisons. Gen Comp Endocrinol, 55 (1): 104-11. [PMID:6611282]

7. Catania A, Rajora N, Capsoni F, Minonzio F, Star RA, Lipton JM. (1996) The neuropeptide alpha-MSH has specific receptors on neutrophils and reduces chemotaxis in vitro. Peptides, 17 (4): 675-9. [PMID:8804079]

8. Chhajlani V. (1996) Distribution of cDNA for melanocortin receptor subtypes in human tissues. Biochem Mol Biol Int, 38 (1): 73-80. [PMID:8932521]

9. Chhajlani V, Wikberg JE. (1996) Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA (FEBS 11553). FEBS Lett, 390 (2): 238. [PMID:8706868]

10. Conde-Frieboes K, Thøgersen H, Lau JF, Sensfuss U, Hansen TK, Christensen L, Spetzler J, Olsen HB, Nilsson C, Raun K et al.. (2012) Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues. J Med Chem, 55 (5): 1969-77. [PMID:22335602]

11. Dinulescu DM, Cone RD. (2000) Agouti and agouti-related protein: analogies and contrasts. J Biol Chem, 275 (10): 6695-8. [PMID:10702221]

12. Hartmeyer M, Scholzen T, Becher E, Bhardwaj RS, Schwarz T, Luger TA. (1997) Human dermal microvascular endothelial cells express the melanocortin receptor type 1 and produce increased levels of IL-8 upon stimulation with alpha-melanocyte-stimulating hormone. J Immunol, 159 (4): 1930-7. [PMID:9257858]

13. Herpin TF, Yu G, Carlson KE, Morton GC, Wu X, Kang L, Tuerdi H, Khanna A, Tokarski JS, Lawrence RM et al.. (2003) Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J Med Chem, 46 (7): 1123-6. [PMID:12646021]

14. Hruby VJ, Lu D, Sharma SD, Castrucci AL, Kesterson RA, al-Obeidi FA, Hadley ME, Cone RD. (1995) Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J Med Chem, 38 (18): 3454-61. [PMID:7658432]

15. Jayawickreme CK, Jayawickreme SP, Lerner MR. (1998) Generation of multiuse peptide libraries for functional screenings. Methods Mol Biol, 87: 107-18. [PMID:9523265]

16. Kadekaro AL, Kavanagh R, Kanto H, Terzieva S, Hauser J, Kobayashi N, Schwemberger S, Cornelius J, Babcock G, Shertzer HG et al.. (2005) alpha-Melanocortin and endothelin-1 activate antiapoptotic pathways and reduce DNA damage in human melanocytes. Cancer Res, 65 (10): 4292-9. [PMID:15899821]

17. Kadekaro AL, Leachman S, Kavanagh RJ, Swope V, Cassidy P, Supp D, Sartor M, Schwemberger S, Babcock G, Wakamatsu K et al.. (2010) Melanocortin 1 receptor genotype: an important determinant of the damage response of melanocytes to ultraviolet radiation. FASEB J, 24 (10): 3850-60. [PMID:20519635]

18. Kask A, Mutulis F, Muceniece R, Pähkla R, Mutule I, Wikberg JE, Rägo L, Schiöth HB. (1998) Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo. Endocrinology, 139 (12): 5006-14. [PMID:9832440]

19. Kiefer LL, Veal JM, Mountjoy KG, Wilkison WO. (1998) Melanocortin receptor binding determinants in the agouti protein. Biochemistry, 37 (4): 991-7. [PMID:9454589]

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