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 |
| 15974575 |
127 |
Peptoid-peptide hybrids as potent novel melanocortin receptor ligands. |
Utrecht University |
| 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 |
| 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 |
| 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 |
| 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 |
| 13678399 |
54 |
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes. |
University of Arizona |
| 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 |
| 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 |
| 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 |
| 12873485 |
150 |
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
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). |
Amgen |
| 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 |
| 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 |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
| 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 |
| 18771254 |
153 |
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents. |
Procter & Gamble Pharmaceuticals |
| 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 |
| 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 |
| 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 |
| 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 |
| 16777413 |
65 |
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor. |
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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 14698163 |
60 |
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core. |
Amgen |
| 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 |
| 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 |
| 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 |
| 32602722 |
8 |
A Venomics Approach Coupled to High-Throughput Toxin Production Strategies Identifies the First Venom-Derived Melanocortin Receptor Agonists. |
Universit£ |
| 26599352 |
35 |
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
Universit£ |
| 12801221 |
16 |
QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes. |
Uppsala University |
| 29679901 |
74 |
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 |
| 29660981 |
122 |
Development of Macrocyclic Peptidomimetics Containing Constrained ?,?-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
University of Naples "Federico Ii |
| 29605997 |
160 |
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
The University of Queensland |
| 29578343 |
32 |
Human?-Defensin 1 and?-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. |
University of Florida |
| 29094944 |
98 |
Design of MC1R Selective?-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation. |
The University of Arizona |
| 28972753 |
82 |
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists. |
University of Copenhagen |
| 19226504 |
5 |
On-chip fragment-based approach for discovery of high-affinity bivalent inhibitors. |
Antibiotics Laboratory |
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