Page last updated: 2024-08-07 13:16:50
Melanocortin receptor 5
A melanocortin receptor 5 that is encoded in the genome of mouse. [OMA:P41149, PRO:DNx]
Synonyms
MC5-R
Research
Bioassay Publications (37)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (2.70) | 18.2507 |
| 2000's | 15 (40.54) | 29.6817 |
| 2010's | 15 (40.54) | 24.3611 |
| 2020's | 6 (16.22) | 2.80 |
Compounds (6)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| msh, 4-nle-7-phe-alpha- | Mus musculus (house mouse) | IC50 | 0.1400 | 1 | 1 |
Drugs with Activation Measurements
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.ACS medicinal chemistry letters, , Feb-12, Volume: 6, Issue:2, 2015
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.ACS medicinal chemistry letters, , Feb-12, Volume: 6, Issue:2, 2015
Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.ACS medicinal chemistry letters, , Mar-12, Volume: 11, Issue:3, 2020
Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.ACS medicinal chemistry letters, , Mar-12, Volume: 11, Issue:3, 2020
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-XaaJournal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.ACS medicinal chemistry letters, , Feb-12, Volume: 6, Issue:2, 2015
Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.ACS medicinal chemistry letters, , Mar-12, Volume: 11, Issue:3, 2020
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Semi-rigid tripeptide agonists of melanocortin receptors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Urea small molecule agonists on mouse melanocortin receptors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
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
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
[no title available]ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Peptoid NPheACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.ACS medicinal chemistry letters, , Mar-12, Volume: 11, Issue:3, 2020
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of MJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
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
[no title available]Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-XaaJournal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
A Macrocyclic Agouti-Related Protein/[NleJournal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at tJournal of medicinal chemistry, , 10-12, Volume: 60, Issue:19, 2017
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanoJournal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Semi-rigid tripeptide agonists of melanocortin receptors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 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
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Urea small molecule agonists on mouse melanocortin receptors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001