Proteins > Melanocyte-stimulating hormone receptor
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Melanocyte-stimulating hormone receptor
A melanocyte-stimulating hormone receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q01726]
Synonyms
MSH-R;
Melanocortin receptor 1;
MC1-R
Research
Bioassay Publications (35)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (14.29) | 18.2507 |
| 2000's | 16 (45.71) | 29.6817 |
| 2010's | 11 (31.43) | 24.3611 |
| 2020's | 3 (8.57) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NHEuropean journal of medicinal chemistry, , May-10, Volume: 151, 2018
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.ACS medicinal chemistry letters, , Feb-12, Volume: 6, Issue:2, 2015
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 2015
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.Journal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 16, Issue:20, 2006
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
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.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NHEuropean journal of medicinal chemistry, , May-10, Volume: 151, 2018
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
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.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
Design of cyclic peptides with agonist activity at melanocortin receptor-4.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 13, Issue:1, 2003
Aryl piperazine melanocortin MC4 receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 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.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
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.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 13, Issue:1, 2003
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 13, Issue:16, 2003
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.Journal of medicinal chemistry, , Aug-15, Volume: 40, Issue:17, 1997
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.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| melanocortin receptor activity | molecular function | Combining with melanocortin to initiate a change in cell activity. [GOC:ai] |
| melanocyte-stimulating hormone receptor activity | molecular function | Combining with melanocyte-stimulating hormone to initiate a change in cell activity. [GOC:jl, PMID:7581459] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:dph, GOC:tb] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| hormone binding | molecular function | Binding to an hormone, a naturally occurring substance secreted by specialized cells that affect the metabolism or behavior of cells possessing functional receptors for the hormone. Hormones may be produced by the same, or different, cell as express the receptor. [GOC:jl] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 14 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| UV protection | biological process | Any process in which an organism or cell protects itself from ultraviolet radiation (UV), which may also result in resistance to repeated exposure to UV. [GOC:jl, GOC:ml] |
| positive regulation of protein kinase A signaling | biological process | Any process that increases the rate, frequency, or extent of protein kinase A signaling. PKA signaling is the series of reactions, mediated by the intracellular serine/threonine kinase protein kinase A, which occurs as a result of a single trigger reaction or compound. [GOC:BHF, GOC:dph, GOC:tb] |
| sensory perception of pain | biological process | The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators] |
| negative regulation of tumor necrosis factor production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of tumor necrosis factor production. [GOC:mah, PMID:10891884, PMID:15560120] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| melanin biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of melanins, pigments largely of animal origin. High molecular weight polymers of indole quinone, they are irregular polymeric structures and are divided into three groups: allomelanins in the plant kingdom and eumelanins and phaeomelanins in the animal kingdom. [GOC:curators] |
| pigmentation | biological process | The accumulation of pigment in an organism, tissue or cell, either by increased deposition or by increased number of cells. [GOC:jl] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| UV-damage excision repair | biological process | A DNA repair process that is initiated by an endonuclease that introduces a single-strand incision immediately 5' of a UV-induced damage site. UV-damage excision repair acts on both cyclobutane pyrimidine dimers (CPDs) and pyrimidine-pyrimidone 6-4 photoproducts (6-4PPs). [GOC:mah, PMID:9619100] |
| positive regulation of protein kinase C signaling | biological process | Any process that increases the frequency, rate, or extent of a series of reactions, mediated by the intracellular serine/threonine kinase protein kinase C, which occurs as a result of a single trigger reaction or compound. [GOC:dph, GOC:tb] |
| positive regulation of feeding behavior | biological process | Any process that activates or increases the frequency, rate or extent of feeding behavior. [GOC:obol] |
| regulation of metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways within a cell or an organism. [GOC:go_curators] |