The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28045525 |
54 |
A Macrocyclic Agouti-Related Protein/[Nle |
University of Minnesota |
26218460 |
264 |
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors. |
University of Arizona |
25699148 |
41 |
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
Vrije Universiteit Brussel |
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. |
Novo Nordisk |
20329799 |
176 |
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. |
Pfizer |
19473029 |
110 |
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
University of Arizona |
18412316 |
52 |
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: discovery of potent and selective hMC5R receptor antagonists. |
University of Arizona |
18032040 |
49 |
Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
18479920 |
68 |
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators. |
Merck Research Laboratories |
18088090 |
72 |
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
University of Arizona |
15771429 |
104 |
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
University of Arizona |
15808454 |
49 |
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists. |
Merck Research Laboratories |
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. |
Merck Research Laboratories |
15482933 |
55 |
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
12904077 |
75 |
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 |
12431055 |
52 |
Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors. |
University of Arizona |
12036373 |
72 |
Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors. |
University of Arizona |
11150170 |
30 |
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. |
University of Arizona |
9216831 |
60 |
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
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. |
University of Michigan Medical Center |
14643340 |
41 |
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype. |
Merck Research Laboratories |
14552781 |
45 |
Aryl piperazine melanocortin MC4 receptor agonists. |
Neurocrine Biosciences |
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. |
Roche Research Center |
11909712 |
124 |
N-alkylaminoacids and their derivatives interact with melanocortin receptors. |
Uppsala University |
22011200 |
24 |
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand. |
H. Lee Moffitt Cancer Center & Research Institute |
21486697 |
17 |
Cyclic lactam hybrida-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
University of Arizona |
21439820 |
43 |
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. |
Merck Research Laboratories |
21277204 |
16 |
Serendipitous discovery of a new class of agonists for the melanocortin 1 and 4 receptors and a new class of cyclophanes. |
Novo Nordisk |
20621473 |
56 |
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists. |
Merck Research Laboratories |
20598533 |
71 |
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands. |
Merck Research Laboratories |
20207541 |
18 |
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist. |
Merck Research Laboratories |
18682322 |
93 |
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands. |
Neurocrine Biosciences |
18417348 |
82 |
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists. |
Neurocrine Biosciences |
17994683 |
55 |
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor. |
Neurocrine Biosciences |
17933528 |
68 |
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
17918824 |
39 |
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 |
17822895 |
110 |
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
17768046 |
70 |
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core. |
Merck |
17618123 |
674 |
Design and synthesis of a library of tertiary amides: evaluation as mimetics of the melanocortins' active core. |
Uppsala University |
17574418 |
117 |
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor. |
Institut Henri Beaufour |
17544282 |
39 |
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity. |
Neurocrine Biosciences |
17455928 |
171 |
Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone. |
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. |
Vrije Universiteit Brussel |
17154518 |
27 |
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
University of Arizona |
16931008 |
72 |
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
University of Arizona |
16824757 |
67 |
Propionylpiperazines as human melanocortin-4 receptor ligands. |
Neurocrine Biosciences |
16777413 |
65 |
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
16697187 |
46 |
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor. |
Neurocrine Biosciences |
16539382 |
136 |
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
University of Arizona |
16364639 |
101 |
Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands. |
Merck Research Laboratories |
16297618 |
32 |
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor. |
Eli Lilly |
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. |
Roche Research Center |
16005624 |
97 |
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif. |
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. |
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. |
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. |
Neurocrine Biosciences |
15863313 |
65 |
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice. |
Neurocrine Biosciences |
15857110 |
96 |
Discovery of a beta-MSH-derived MC-4R selective agonist. |
Eli Lilly |
15745810 |
39 |
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides. |
Amgen |
15664867 |
33 |
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines. |
Neurocrine Biosciences |
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. |
Neurocrine Biosciences |
15357964 |
90 |
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
15317471 |
42 |
New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of"THIQ". |
Uppsala University |
15267247 |
55 |
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists. |
Neurocrine Biosciences |
14736255 |
68 |
Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor. |
Eli Lilly |
14584947 |
108 |
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 |
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. |
Roche Research Center |
12646021 |
35 |
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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. |
Merck |
11909711 |
86 |
Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors. |
Uppsala University |
11606131 |
92 |
Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro. |
Merck Research Laboratories |