The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
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 |
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. |
Glaxosmithkline |
19635667 |
110 |
Semi-rigid tripeptide agonists of melanocortin receptors. |
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. |
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 |
18078748 |
41 |
Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists. |
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. |
University Of Arizona |
16678415 |
21 |
Design of cyclic peptides with agonist activity at melanocortin receptor-4. |
Asahi Kasei Pharma |
15771429 |
104 |
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues. |
University Of Arizona |
15911261 |
62 |
Design, synthesis, and evaluation of proline based melanocortin receptor ligands. |
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. |
Merck Research Laboratories |
15482933 |
55 |
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor. |
Neurocrine Biosciences |
14998337 |
68 |
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach. |
University Of Arizona |
13678399 |
54 |
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes. |
University Of Arizona |
9276019 |
11 |
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity. |
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 |
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. |
University Of Arizona |
14552781 |
45 |
Aryl piperazine melanocortin MC4 receptor agonists. |
Neurocrine Biosciences |
12873485 |
150 |
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
University Of Cincinnati |
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 |
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. |
Roche Research Center |
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 |
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 |
18771254 |
153 |
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents. |
Procter & Gamble Pharmaceuticals |
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 |
17964151 |
107 |
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for 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 |
17574418 |
117 |
Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor. |
Institut Henri Beaufour |
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 |
16854081 |
216 |
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach. |
Procter & Gamble Pharmaceuticals |
16824757 |
67 |
Propionylpiperazines as human melanocortin-4 receptor ligands. |
Neurocrine Biosciences |
16766182 |
108 |
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists. |
Procter & Gamble Pharmaceuticals |
16539382 |
136 |
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
University Of Arizona |
16376076 |
40 |
Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists. |
Procter & Gamble Pharmaceuticals |
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 |
16203134 |
37 |
Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2. |
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. |
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 |
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 |
15341935 |
138 |
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists. |
University Of Cincinnati |
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 |
12668001 |
17 |
Peptoid mimics of agouti related protein. |
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. |
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 |
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. |
Roche Research Center |
12593660 |
23 |
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist. |
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. |
Merck |
11909711 |
86 |
Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors. |
Uppsala University |
7473600 |
11 |
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities. |
University Of Arizona |
19354253 |
13 |
Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase. |
Vanderbilt University |