BindingDB logo
myBDB logout

114 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28045525 54 A Macrocyclic Agouti-Related Protein/[NleEBI University of Minnesota
26959173 85 An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.EBI University of Minnesota
26433448 10 A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.EBI University of Minnesota
26218460 264 Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.EBI University of Arizona
26005535 28 Synthesis and Pharmacology ofa/(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.EBI University of Minnesota
25898270 88 Discovery of a-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.EBI University of Minnesota
25699148 41 Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.EBI Vrije Universiteit Brussel
25699138 38 Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.EBI University of Minnesota
25347033 93 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.EBI University of Cergy-Pontoise
24517312 98 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).EBI University of Florida
23432160 78 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 melanocortin-4 receptor (mMC4R).EBI University of Florida
22335602 93 Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selectivea-melanocyte-stimulating hormone (a-MSH) analogues.EBI Novo Nordisk A/S
20329799 176 Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.EBI Pfizer Global Research and Development
20172734 22 A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity.EBI GlaxoSmithKline
19635667 110 Semi-rigid tripeptide agonists of melanocortin receptors.EBI University of Cincinnati
19473029 110 Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.EBI University of Arizona
18800761 69 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.EBI University of Florida
18412316 52 Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.EBI University of Arizona
18220330 28 Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.EBI The Hebrew University of Jerusalem
18271518 43 The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.EBI University of Florida
18032040 49 Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
18078748 41 Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.EBI Nanyang Technological University
18088090 72 Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.EBI University of Arizona
15615519 42 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.EBI University of Florida
16678415 21 Design of cyclic peptides with agonist activity at melanocortin receptor-4.EBI Asahi Kasei Pharma Corporation
15857138 64 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.EBI University of Florida
15828845 93 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.EBI University of Florida
15771429 104 Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.EBI University of Arizona
15911261 62 Design, synthesis, and evaluation of proline based melanocortin receptor ligands.EBI Procter& Gamble Pharmaceuticals
15582434 37 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.EBI Merck Research Laboratories
15482933 55 Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
15084118 79 Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.EBI University of Florida
14998337 68 De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.EBI University of Arizona
13678399 54 Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.EBI University of Arizona
12477357 96 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.EBI University of Florida
12086493 120 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.EBI University of Florida
12061882 83 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.EBI University of Florida
11405661 61 Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.EBI University of Florida
9276019 11 beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.EBI University of Arizona
9216831 60 Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.EBI University of Michigan Medical Center
9171884 52 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.EBI University of Michigan Medical Center
7658432 46 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.EBI University of Arizona
14643357 29 Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.EBI University of Florida
14552781 45 Aryl piperazine melanocortin MC4 receptor agonists.EBI Neurocrine Biosciences Inc.
12873485 150 Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).EBI University of Cincinnati
12824029 21 Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).EBI Amgen Inc.
12781199 64 Urea small molecule agonists on mouse melanocortin receptors.EBI University of Florida
12467633 58 Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.EBI Roche Research Center
11909712 124 N-alkylaminoacids and their derivatives interact with melanocortin receptors.EBI Uppsala University
12161144 23 Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.EBI Roche Research Center
22011200 24 Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.EBI H. Lee Moffitt Cancer Center& Research Institute
21873053 5 Improved synthesis and biological evaluation of chelator-modifieda-MSH analogs prepared by copper-free click chemistry.EBI The University of Iowa
21486697 17 Cyclic lactam hybrida-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.EBI University of Arizona
21439820 43 Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.EBI Merck Research Laboratories
21306168 36 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.EBI University of Florida
21277204 16 Serendipitous discovery of a new class of agonists for the melanocortin 1 and 4 receptors and a new class of cyclophanes.EBI Novo Nordisk
20728365 1 Replacement of the Lys linker with an Arg linker resulting in improved melanoma uptake and reduced renal uptake of Tc-99m-labeled Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide.EBI University of New Mexico
20598533 71 Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.EBI Merck Research Laboratories
20207541 18 Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.EBI Merck Research Laboratories
20056544 50 The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: the melanocortin agonist paradigm.EBI The Hebrew University of Jerusalem
18771254 153 Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.EBI Procter & Gamble Pharmaceuticals
18417348 82 Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.EBI Neurocrine Biosciences, Inc.
17994683 55 Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
17964151 107 Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.EBI Neurocrine Biosciences Inc.
17933528 68 Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
17618123 674 Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core.EBI Uppsala University
17574418 117 Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.EBI Institut Henri Beaufour
17455928 171 Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.EBI Merck Research Laboratories
17314042 40 Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.EBI Vrije Universiteit Brussel
17154518 27 Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.EBI University of Arizona
16931008 72 Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.EBI University of Arizona
16854081 216 Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.EBI Procter & Gamble Pharmaceuticals
16824757 67 Propionylpiperazines as human melanocortin-4 receptor ligands.EBI Neurocrine Biosciences, Inc.
16766182 108 Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.EBI Procter & Gamble Pharmaceuticals
16539382 136 Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.EBI University of Arizona
16376076 40 Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.EBI Procter & Gamble Pharmaceuticals
16364639 101 Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.EBI Merck Research Laboratories
16297618 32 Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.EBI Lilly Research Laboratories
16203134 37 Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2.EBI Roche Research Center
16169218 30 Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides.EBI Roche Research Center
16005624 97 Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif.EBI Merck Research Laboratories
15982875 46 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 subtype-4 receptor agonist.EBI Merck Research Laboratories
15951175 28 1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.EBI Merck Research Laboratories
15950470 69 Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
15863313 65 A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.EBI Neurocrine Biosciences, Inc.
15857110 96 Discovery of a beta-MSH-derived MC-4R selective agonist.EBI Lilly Research Laboratories
15615531 30 4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.EBI Neurocrine Biosciences, Inc.
15509165 6 Structural characterization and pharmacology of a potent (Cys101-Cys119, Cys110-Cys117) bicyclic agouti-related protein (AGRP) melanocortin receptor antagonist.EBI University of Florida
15357964 90 Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
15341935 138 End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.EBI University of Cincinnati
15317471 42 New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".EBI Uppsala University
15267247 55 Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.EBI Neurocrine Biosciences, Inc.
14736255 68 Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.EBI Lilly Research Laboratories
14698163 60 Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.EBI Amgen Inc.
12668001 17 Peptoid mimics of agouti related protein.EBI University of California
12657270 57 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.EBI Roche Research Center
12646021 35 Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12639550 55 Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution.EBI Roche Research Center
12593660 23 Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.EBI University of Arizona
12361385 34 Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.EBI Merck & Co.
12086490 5 Modification of the structure of a metallopeptide: synthesis and biological evaluation of (111)In-labeled DOTA-conjugated rhenium-cyclized alpha-MSH analogues.EBI University of Missouri-Columbia
11909711 86 Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.EBI Uppsala University
11708914 4 Novel agouti-related-protein-based melanocortin-1 receptor antagonist.EBI University of Florida
10543881 10 Compounds that activate the mouse melanocortin-1 receptor identified by screening a small molecule library based upon the beta-turn.EBI Oregon Health Sciences University
7473600 11 Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.EBI University of Arizona
8884876 47 Characterisation of the melanocortin 4 receptor by radioligand binding.BDB Uppsala University
7774675 35 Characterisation of melanocortin receptor subtypes by radioligand binding analysis.BDB Uppsala