Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction (Q28271756)

Nature Reviews Drug Discovery

Europe PubMed Central

title

Targeting melanocortin receptors: an approach to treat weight disorders and sexual dysfunction (English)

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1

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author name string

Felikss Mutulis

series ordinal

2

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language of work or name

English

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publication date

April 2008

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published in

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volume

7

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issue

4

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page(s)

307-23

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cites work

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The central melanocortin system directly controls peripheral lipid metabolism

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Dopamine-deficient mice are severely hypoactive, adipsic, and aphagic

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The MC4 receptor mediates alpha-MSH induced release of nucleus accumbens dopamine

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Melanocortin-4 receptor-deficient mice are not hypertensive or salt-sensitive despite obesity, hyperinsulinemia, and hyperleptinemia.

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Hypertension and the metabolic syndrome

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Gamma-MSH, sodium metabolism, and salt-sensitive hypertension

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Dietary sodium intake modulates pituitary proopiomelanocortin mRNA abundance

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Modulation by dietary sodium intake of melanocortin 3 receptor mRNA and protein abundance in the rat kidney

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Cardiovascular effects of adrenocorticotropin microinjections into the rostral ventrolateral medullary pressor area of the rat.

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Suppression of γ-Melanocyte–Stimulating Hormone Secretion Is Accompanied by Salt-Sensitive Hypertension in the Rat

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Nerve growth factor regulates HCO3- absorption in thick ascending limb: modifying effects of vasopressin.

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Salt sensitivity: a consequence of the metabolic syndrome?

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Central receptors mediating the cardiovascular actions of melanocyte stimulating hormones

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Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage

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

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Stimulation of progesterone release and estrous behavior by ACTH in ovariectomized rodents

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ACTH- and alpha-MSH-induced grooming, stretching, yawning and penile erection in male rats: site of action in the brain and role of melanocortin receptors

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Behavioral effects of alpha-MSH and MCH after central administration in the female rat.

31 March 2020

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31 March 2020

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A role for the melanocortin 4 receptor in sexual function

31 March 2020

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Differential influence of a selective melanocortin MC4 receptor antagonist (HS014) on melanocortin-induced behavioral effects in rats.

31 March 2020

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Melanotan-II: Investigation of the inducer and facilitator effects on penile erection in anaesthetized rat.

31 March 2020

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Ac-nle-c[asp-his-dphe-arg-trp-lys]-nh2 induces penile erection via brain and spinal melanocortin receptors

31 March 2020

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Effects of alpha-melanocyte-stimulating hormone on magnocellular oxytocin neurones and their activation at intromission in male rats.

31 March 2020

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Alpha-melanocyte-stimulating hormone stimulates oxytocin release from the dendrites of hypothalamic neurons while inhibiting oxytocin release from their terminals in the neurohypophysis.

31 March 2020

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CD38 regulates oxytocin secretion and complex social behavior.

31 March 2020

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Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist

31 March 2020

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Hypoactive sexual desire disorder: an underestimated condition in men.

31 March 2020

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Testosterone therapy in women: a review

31 March 2020

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Let's talk about sex--and drugs

31 March 2020

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Obesity-associated mutations in the melanocortin 4 receptor provide novel insights into its function

31 March 2020

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Obesity due to proopiomelanocortin deficiency: three new cases and treatment trials with thyroid hormone and ACTH4-10.

31 March 2020

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A missense mutation disrupting a dibasic prohormone processing site in pro-opiomelanocortin (POMC) increases susceptibility to early-onset obesity through a novel molecular mechanism

31 March 2020

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Association between an agouti-related protein gene polymorphism and anorexia nervosa

31 March 2020

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Ala67Thr polymorphism in the Agouti-related peptide gene is associated with inherited leanness in humans

31 March 2020

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Two ethnic-specific polymorphisms in the human Agouti-related protein gene are associated with macronutrient intake

31 March 2020

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31 March 2020

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A novel melanocortin 3 receptor gene (MC3R) mutation associated with severe obesity

31 March 2020

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The relationship between active ghrelin levels and human obesity involves alterations in resting energy expenditure

31 March 2020

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Inactivation and intracellular retention of the human I183N mutated melanocortin 3 receptor associated with obesity

31 March 2020

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Melanocortin-3-receptor gene variants in morbid obesity

31 March 2020

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The Val81 missense mutation of the melanocortin 3 receptor gene, but not the 1908c/T nucleotide polymorphism in lamin A/C gene, is associated with hyperleptinemia and hyperinsulinemia in obese Greek caucasians.

31 March 2020

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Gene variants and binge eating as predictors of comorbidity and outcome of treatment in severe obesity

31 March 2020

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Obesity-associated mutations in the human melanocortin-4 receptor gene

31 March 2020

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Binge-eating episodes are not characteristic of carriers of melanocortin-4 receptor gene mutations.

31 March 2020

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Functional analyses of melanocortin-4 receptor mutations identified from patients with binge eating disorder and nonobese or obese subjects

31 March 2020

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The 103I variant of the melanocortin 4 receptor is associated with low serum triglyceride levels

31 March 2020

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The V103I polymorphism of the MC4R gene and obesity: population based studies and meta-analysis of 29 563 individuals

31 March 2020

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Association of the 103I MC4R allele with decreased body mass in 7937 participants of two population based surveys

31 March 2020

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Targeted disruption of the melanocortin-4 receptor results in obesity in mice

31 March 2020

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

31 March 2020

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New aspects on the melanocortins and their receptors

31 March 2020

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Inverse agonism gains weight

31 March 2020

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Modeling and docking of the three-dimensional structure of the human melanocortin 4 receptor.

31 March 2020

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A three dimensional model for the interaction of MSH with the melanocortin-1 receptor.

31 March 2020

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Modeling of the three-dimensional structure of the human melanocortin 1 receptor, using an automated method and docking of a rigid cyclic melanocyte-stimulating hormone core peptide.

31 March 2020

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Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists

31 March 2020

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Proteochemometric mapping of the interaction of organic compounds with melanocortin receptor subtypes

31 March 2020

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Improved approach for proteochemometrics modeling: application to organic compound--amine G protein-coupled receptor interactions

31 March 2020

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4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity

31 March 2020

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Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position

31 March 2020

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Potent and prolonged acting cyclic lactam analogues of alpha-melanotropin: design based on molecular dynamics

31 March 2020

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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

31 March 2020

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Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra

31 March 2020

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Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction

31 March 2020

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Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response

31 March 2020

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An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist

31 March 2020

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Potent and selective MC-4 receptor agonists based on a novel disulfide scaffold

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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Assessment of a small molecule melanocortin-4 receptor-specific agonist on energy homeostasis

31 March 2020

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Cardiovascular responses to melanocortin 4-receptor stimulation in conscious unrestrained normotensive rats

31 March 2020

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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines

31 March 2020

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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice

31 March 2020

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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 melanocorti

31 March 2020

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Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor

31 March 2020

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Propionylpiperazines as human melanocortin-4 receptor ligands.

31 March 2020

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Metabolic activation of a 1,3-disubstituted piperazine derivative: evidence for a novel ring contraction to an imidazoline

31 March 2020

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Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype

31 March 2020

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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

31 March 2020

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Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists

31 March 2020

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Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.

31 March 2020

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Design, synthesis, and evaluation of proline based melanocortin receptor ligands

31 March 2020

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Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists

31 March 2020

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

31 March 2020

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Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists

31 March 2020

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

31 March 2020

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Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity

31 March 2020

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Cross down-regulation of leptin and insulin receptor expression and signalling in a human neuronal cell line.

31 March 2020

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The therapeutic potential of leptin

31 March 2020

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Leptin predicts a worsening of the features of the metabolic syndrome independently of obesity

31 March 2020

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Aged-obese rats exhibit robust responses to a melanocortin agonist and antagonist despite leptin resistance

31 March 2020

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Does obesity induce resistance to the long-term cardiovascular and metabolic actions of melanocortin 3/4 receptor activation?

31 March 2020

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Leptin resistance in obesity is characterized by decreased sensitivity to proopiomelanocortin products.

31 March 2020

1 reference

Role of adrenergic activity in pressor responses to chronic melanocortin receptor activation

31 March 2020

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Overweight humans are resistant to the weight-reducing effects of melanocortin4-10.

31 March 2020

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A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice.

31 March 2020

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Melanocortin 3 receptors control crystal-induced inflammation

31 March 2020

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The melanocortin peptide HP228 displays protective effects in acute models of inflammation and organ damage.

31 March 2020

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Neuroprotective effects of melanocortins in experimental spinal cord injury. An experimental study in the rat using topical application of compounds with varying affinity to melanocortin receptors

31 March 2020

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Selective melanocortin MC4 receptor blockage reduces immobilization stress-induced anorexia in rats

31 March 2020

1 reference

The use of melanocortin antagonists in cachexia of chronic disease

31 March 2020

1 reference

Anticatabolic properties of melanocortin-4 receptor antagonists

31 March 2020

1 reference

Central infusion of the melanocortin receptor antagonist agouti-related peptide (AgRP(83-132)) prevents cachexia-related symptoms induced by radiation and colon-26 tumors in mice

31 March 2020

1 reference

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

31 March 2020

1 reference

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.

31 March 2020

1 reference

Polyclonal antibodies against human melanocortin MC1 receptor: preliminary immunohistochemical localisation of melanocortin MC1 receptor to malignant melanoma cells

31 March 2020

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The neuropeptide alpha-MSH has specific receptors on neutrophils and reduces chemotaxis in vitro

31 March 2020

1 reference

MC(1) receptors are constitutively expressed on leucocyte subpopulations with antigen presenting and cytotoxic functions

31 March 2020

1 reference

Expression of melanocortin 1 receptor in periaqueductal gray matter

31 March 2020

1 reference

Increased sensitivity to thermal pain and reduced subcutaneous lidocaine efficacy in redheads

31 March 2020

1 reference

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

31 March 2020

1 reference

Localization of ACTH receptor mRNA by in situ hybridization in mouse adrenal gland

31 March 2020

1 reference

Major pharmacological distinction of the ACTH receptor from other melanocortin receptors

31 March 2020

1 reference

Identification of a receptor for gamma melanotropin and other proopiomelanocortin peptides in the hypothalamus and limbic system

31 March 2020

1 reference

Autoradiographic discrimination of melanocortin receptors indicates that the MC3 subtype dominates in the medial rat brain

31 March 2020

1 reference

Quantitative measurement of the levels of melanocortin receptor subtype 1, 2, 3 and 5 and pro-opio-melanocortin peptide gene expression in subsets of human peripheral blood leucocytes.

31 March 2020

1 reference

Melanocortin receptor type 3 as a potential target for anti-inflammatory therapy

31 March 2020

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The MC3 receptor binding affinity of melanocortins correlates with the nitric oxide production inhibition in mice brain inflammation model

31 March 2020

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Melanocortin 4 receptor is expressed in the dorsal root ganglions and down-regulated in neuropathic rats.

31 March 2020

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Melanocortin receptor 4 is induced in nerve-injured motor and sensory neurons of mouse

31 March 2020

1 reference

Expression of melanocortin-5 receptor in secretory epithelia supports a functional role in exocrine and endocrine glands

31 March 2020

1 reference

Cloning, expression, and tissue distribution of a fifth melanocortin receptor subtype

31 March 2020

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31 March 2020

1 reference

Interactions of alpha-melanotropin and agouti on B16 melanoma cells: evidence for inverse agonism of agouti

31 March 2020

1 reference

Characterisation of the melanocortin 4 receptor by radioligand binding

31 March 2020

1 reference

β-MSH: a functional ligand that regulated energy homeostasis via hypothalamic MC4-R?

31 March 2020

1 reference

Characterisation of melanocortin receptor subtypes by radioligand binding analysis

31 March 2020

1 reference

Melanocortin receptors form constitutive homo- and heterodimers

31 March 2020

1 reference

Autosomal-dominant mode of inheritance of a melanocortin-4 receptor mutation in a patient with severe early-onset obesity is due to a dominant-negative effect caused by receptor dimerization.

31 March 2020

1 reference

Kinetic evidence for tandemly arranged ligand binding sites in melanocortin 4 receptor complexes

31 March 2020

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Co-operative regulation of ligand binding to melanocortin receptor subtypes: evidence for interacting binding sites

31 March 2020

1 reference

Regulation of melanocortin-4 receptor signaling: agonist-mediated desensitization and internalization

31 March 2020

1 reference

Functional selectivity of melanocortin 4 receptor peptide and nonpeptide agonists: evidence for ligand-specific conformational states.

31 March 2020

1 reference

The natural inverse agonist agouti-related protein induces arrestin-mediated endocytosis of melanocortin-3 and -4 receptors

31 March 2020

1 reference

A role for syndecan-3 in the melanocortin regulation of energy balance

31 March 2020

1 reference

Transgenic expression of syndecan-1 uncovers a physiological control of feeding behavior by syndecan-3.

31 March 2020

1 reference

Syndecans: new kids on the signaling block

31 March 2020

1 reference

31 March 2020

1 reference

Mahogany/attractin: en route from phenotype to function

31 March 2020

1 reference

Attractin' more attention - new pieces in the obesity puzzle?

31 March 2020

1 reference

Prediction of indirect interactions in proteins

31 March 2020

1 reference

Proteochemometric modeling reveals the interaction site for Trp9 modified alpha-MSH peptides in melanocortin receptors.

31 March 2020

1 reference

Melanocortin-3 receptor mRNA expression in pro-opiomelanocortin neurones of the rat arcuate nucleus.

31 March 2020

1 reference

Melanocortins and agouti-related protein modulate the excitability of two arcuate nucleus neuron populations by alteration of resting potassium conductances.

31 March 2020

1 reference

Expression of melanocortin MC3 and MC4 receptor mRNAs by neuropeptide Y neurons in the rat arcuate nucleus.

31 March 2020

1 reference

Hypothalamic interactions between neuropeptide Y, agouti-related protein, cocaine- and amphetamine-regulated transcript and alpha-melanocyte-stimulating hormone in vitro in male rats

31 March 2020

1 reference

Regulation of neuropeptide Y release from hypothalamic slices by melanocortin-4 agonists and leptin

31 March 2020

1 reference

PT-141: a melanocortin agonist for the treatment of sexual dysfunction

31 March 2020

1 reference

A novel and selective beta-melanocyte-stimulating hormone-derived peptide agonist for melanocortin 4 receptor potently decreased food intake and body weight gain in diet-induced obese rats

31 March 2020

1 reference

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

31 March 2020

1 reference

Preparation of human Melanocortin-4 receptor agonist libraries: linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2.

31 March 2020

1 reference

End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands

31 March 2020

1 reference

2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.

31 March 2020

1 reference

beta-alanine dipeptides as MC4R agonists

31 March 2020

1 reference

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

31 March 2020

1 reference

Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines

31 March 2020

1 reference

Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor

31 March 2020

1 reference

Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor

31 March 2020

1 reference

Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.

31 March 2020

1 reference

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor

31 March 2020

1 reference

Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor

31 March 2020

1 reference

New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ".

31 March 2020

1 reference

Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives

31 March 2020

1 reference

Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor

31 March 2020

1 reference

Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor

31 March 2020

1 reference

Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif

31 March 2020

1 reference

A role for the Agouti-Related Protein promoter in obesity and type 2 diabetes

31 March 2020

1 reference

Functional dimorphism of two hAgRP promoter SNPs in linkage disequilibrium

31 March 2020

1 reference

A polymorphism in the human agouti-related protein is associated with late-onset obesity

31 March 2020

1 reference

Functional analysis of the Ala67Thr polymorphism in agouti related protein associated with anorexia nervosa and leanness

31 March 2020

1 reference

The role of melanocortin receptors in sexual behavior in female rats

31 March 2020

1 reference

Hypothalamic melanocortin system regulates sympathetic nerve activity in brown adipose tissue

31 March 2020

1 reference

7 January 2021

Dietary sodium modulates mRNA abundance of enzymes involved in pituitary processing of proopiomelanocortin

1 reference

7 January 2021

Chemogenomics in drug discovery

1 reference

7 January 2021

Proteochemometrics: A Tool for Modeling the Molecular Interaction Space

1 reference

7 January 2021

release_ylfn6x3ylzc2lnisulruebot74

Identifiers

DOI

10.1038/NRD2331

0 references

Fatcat ID

1 reference

Fatcat

https://api.fatcat.wiki/v0/release/ylfn6x3ylzc2lnisulruebot74

24 November 2022