85 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
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
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.
Glaxosmithkline
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 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
Design of cyclic peptides with agonist activity at melanocortin receptor-4.
Asahi Kasei Pharma
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
University of Arizona
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
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
University of Arizona
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
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
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
University of Cincinnati
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
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.
Roche Research Center
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
H. Lee Moffitt Cancer Center & Research Institute
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
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
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
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
Institut Henri Beaufour
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
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Procter & Gamble Pharmaceuticals
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
Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2.
Roche Research Center
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
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
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
Eli Lilly
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
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.
Roche Research Center
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.
University of Arizona
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
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
University of Arizona
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
On-chip fragment-based approach for discovery of high-affinity bivalent inhibitors.
Antibiotics Laboratory