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Melanocortin receptor 3
A melanocortin receptor 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41968]
Synonyms
MC3-R
Research
Bioassay Publications (34)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (8.82) | 18.2507 |
| 2000's | 16 (47.06) | 29.6817 |
| 2010's | 11 (32.35) | 24.3611 |
| 2020's | 4 (11.76) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
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
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.Journal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
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
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
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.Journal of medicinal chemistry, , Dec-24, Volume: 58, Issue:24, 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
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 a new class of small molecule peptide mimetics targeting the melanocortin receptors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 16, Issue:20, 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
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 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
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
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
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
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
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtBioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
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
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
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 relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
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
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
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
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
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
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
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
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.Journal of medicinal chemistry, , Aug-14, Volume: 46, Issue:17, 2003
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 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
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 5 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] |
| neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
| peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
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 |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| 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] |
Involved In
This protein is involved in 11 target(s):
| Target | Category | Definition |
|---|
| regulation of heart rate | biological process | Any process that modulates the frequency or rate of heart contraction. [GOC:dph, GOC:tb, PMID:10358008] |
| 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] |
| phospholipase C-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 phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
| homoiothermy | biological process | Any homoeostatic process in which an organism maintains its internal body temperature at a relatively constant value. This is achieved by using metabolic processes to counteract fluctuations in the temperature of the environment. [ISBN:0192801023] |
| locomotor rhythm | biological process | The rhythm of the locomotor activity of an organism during its 24 hour activity cycle. [GOC:go_curators] |
| sodium ion homeostasis | biological process | Any process involved in the maintenance of an internal steady state of sodium ions within an organism or cell. [GOC:ai, GOC:jid, GOC:mah] |
| regulation of feeding behavior | biological process | Any process that modulates the rate, frequency or extent of the behavior associated with the intake of food. [GOC:BHF, GOC:dph, GOC:tb] |
| 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] |