105 articles for thisTarget
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Article Title
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Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
University of Arizona
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
Vrije Universiteit Brussel
Peptoid-peptide hybrids as potent novel melanocortin receptor ligands.
Utrecht University
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selectivea-melanocyte-stimulating hormone (a-MSH) analogues.
Novo Nordisk
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
Pfizer
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
University of Arizona
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists.
University of Arizona
Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Merck Research Laboratories
Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.
Nanyang Technological University
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
University of Arizona
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
University of Arizona
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Merck Research Laboratories
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.
Procter & Gamble Pharmaceuticals
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.
Merck Research Laboratories
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
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.
University of Arizona
Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.
University of Arizona
Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors.
University of Arizona
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
University of Arizona
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
University of Michigan Medical Center
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.
University of Michigan Medical Center
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.
University of Arizona
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.
Merck Research Laboratories
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
University of Cincinnati
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).
Amgen
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.
Roche Research Center
N-alkylaminoacids and their derivatives interact with melanocortin receptors.
Uppsala University
Cyclic lactam hybrida-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
University of Arizona
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Merck Research Laboratories
Serendipitous discovery of a new class of agonists for the melanocortin 1 and 4 receptors and a new class of cyclophanes.
Novo Nordisk
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Merck Research Laboratories
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Merck Research Laboratories
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
Merck Research Laboratories
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.
Procter & Gamble Pharmaceuticals
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Neurocrine Biosciences
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Neurocrine Biosciences
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Neurocrine Biosciences
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
Neurocrine Biosciences
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Neurocrine Biosciences
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Merck
Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core.
Uppsala University
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
Institut Henri Beaufour
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Neurocrine Biosciences
Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.
Merck Research Laboratories
Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.
Vrije Universiteit Brussel
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
University of Arizona
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
University of Arizona
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.
Procter & Gamble Pharmaceuticals
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Procter & Gamble Pharmaceuticals
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Neurocrine Biosciences
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
Universit£
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
University of Arizona
Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Procter & Gamble Pharmaceuticals
Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.
Merck Research Laboratories
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.
Eli Lilly
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.
Roche Research Center
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif.
Merck Research Laboratories
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.
Merck Research Laboratories
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.
Merck Research Laboratories
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Neurocrine Biosciences
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Amgen
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
The University of Queensland
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Neurocrine Biosciences
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.
Neurocrine Biosciences
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Neurocrine Biosciences
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.
University of Cincinnati
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ".
Uppsala University
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
Neurocrine Biosciences
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
The University of Queensland
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
Eli Lilly
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Amgen
Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.
University of Arizona
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure?.
Vrije Universiteit Brussel
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.
Roche Research Center
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.
Bristol-Myers Squibb Pharmaceutical Research Institute
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.
Merck
Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.
Uppsala University
Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro.
Merck Research Laboratories
A Venomics Approach Coupled to High-Throughput Toxin Production Strategies Identifies the First Venom-Derived Melanocortin Receptor Agonists.
Universit£
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
Universit£
QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes.
Uppsala University
Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
University of Arizona
Development of Macrocyclic Peptidomimetics Containing Constrained ?,?-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
University of Naples "Federico Ii
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
The University of Queensland
Human?-Defensin 1 and?-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
University of Florida
Design of MC1R Selective?-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation.
The University of Arizona
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
University of Copenhagen
