(Q24653947)

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Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor

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Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor (English)

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author name string

Alexander V Mayorov

1

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Minying Cai

2

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Erin S Palmer

3

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Matthew M Dedek

4

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James P Cain

5

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April R Van Scoy

6

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Bahar Tan

7

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Josef Vagner

8

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Dev Trivedi

9

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Victor J Hruby

10

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language of work or name

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publication date

24 January 2008

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Journal of Medicinal Chemistry

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51

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2

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187-95

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Melanocortin receptors, melanotropic peptides and penile erection

1 reference

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7 April 2017

Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor

1 reference

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7 April 2017

The melanocortin-1 receptor gene mediates female-specific mechanisms of analgesia in mice and humans

1 reference

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7 April 2017

A role for the melanocortin 4 receptor in sexual function

1 reference

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7 April 2017

Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein

1 reference

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7 April 2017

Melanocortin-5 receptor deficiency reduces a pheromonal signal for aggression in male mice

1 reference

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7 April 2017

Melanocortin-5 receptor deficiency promotes defensive behavior in male mice

1 reference

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7 April 2017

Structure−Activity Relationships of γ-MSH Analogues at the Human Melanocortin MC3, MC4, and MC5 Receptors. Discovery of Highly Selective hMC3R, hMC4R, and hMC5R Analogues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

7 April 2017

The melanocortin system

1 reference

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7 April 2017

Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro

1 reference

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7 April 2017

Molecular determinants of ligand binding to the human melanocortin-4 receptor

1 reference

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7 April 2017

Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study

1 reference

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7 April 2017

Discovery of novel melanocortin4receptor selective MSH analogues

1 reference

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7 April 2017

Exocrine gland dysfunction in MC5-R-deficient mice: evidence for coordinated regulation of exocrine gland function by melanocortin peptides

1 reference

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7 April 2017

Role of melanocortinergic neurons in feeding and the agouti obesity syndrome

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

7 April 2017

Distribution of cDNA for melanocortin receptor subtypes in human tissues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

7 April 2017

Molecular cloning, expression, and gene localization of a fourth melanocortin receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

7 April 2017

Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

7 April 2017

Novel selective human melanocortin-3 receptor ligands: use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Effects of macrocycle size and rigidity on melanocortin receptor-1 and -5 selectivity in cyclic lactam alpha-melanocyte-stimulating hormone analogs

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

The regulation of food intake by selective stimulation of the type 3 melanocortin receptor (MC3R).

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Discovery of a beta-MSH-derived MC-4R selective agonist

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Neuropeptide Y, alpha-melanocyte-stimulating hormone, and monoamines in food intake regulation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

A predictive pharmacophore model of human melanocortin-4 receptor as derived from the solution structures of cyclic peptides

1 reference

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28 September 2017

Biological and conformational study of beta-substituted prolines in MT-II template: steric effects leading to human MC5 receptor selectivity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Solution structures of cyclic melanocortin agonists and antagonists by NMR.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

The central melanocortin system and the integration of short- and long-term regulators of energy homeostasis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Recent developments in our understanding of melanocortin system in the regulation of food intake

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

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.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Discovery and in vivo evaluation of new melanocortin-4 receptor-selective peptides.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

The role of melanocortin peptides and receptors in regulation of energy balance

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Neuropathic pain: a possible role for the melanocortin system?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

ACTH-induced excessive grooming in the rat.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

Binding and cAMP studies of melanotropin peptides with the cloned human peripheral melanocortin receptor, hMC1R.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

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 recep

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 September 2017

pA, a new scale for the measurement of drug antagonism

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

30 May 2018

Induction of sexual excitement by the action of adrenocorticotrophic hormone in brain

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

30 May 2018

Corticotropin inhibits food intake in rats.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

30 May 2018

Inhibition of feeding by ACTH-(1-24): behavioral and pharmacological aspects

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

30 May 2018

Color-monitored solid-phase multiple peptide synthesis under low-pressure continuous-flow conditions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

30 May 2018

Potent and selective peptide agonists of alpha-melanocyte stimulating hormone (alphaMSH) action at human melanocortin receptor 5; their synthesis and biological evaluation in vitro

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Potent and selective agonists of alpha-melanotropin (alphaMSH) action at human melanocortin receptor 5; linear analogs of alpha-melanotropin

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Central receptors mediating the cardiovascular actions of melanocyte stimulating hormones

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

The role of the DRY motif of human MC4R for receptor activation

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

beta-alanine dipeptides as MC4R agonists

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Extensive structure–activity studies of lactam derivatives of MT‐II and SHU‐9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

MC3-R as a novel target for antiinflammatory therapy.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

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 ago

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Potent and selective peptide agonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Melanocortin antagonists define two distinct pathways of cardiovascular control by alpha- and gamma-melanocyte-stimulating hormones.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2587288

28 November 2018

Effect of an alpha-melanocyte stimulating hormone analog on penile erection and sexual desire in men with organic erectile dysfunction

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Color test for detection of free terminal amino groups in the solid-phase synthesis of peptides

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Proceedings of the 5th International Melanocortin Meeting. August 25-28, 2002. Sunriver, Oregon, USA

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Design of cyclic peptides with agonist activity at melanocortin receptor-4

1 reference

https://pubmed.ncbi.nlm.nih.gov/18088090

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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10.1021/JM070461W

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