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Melanocortin ligands: 30 years of structure-activity relationship (SAR) studies

Medicinal research reviews, 2004-05, Vol.24 (3), p.325-356

2004

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The melanocortin pathway and energy homeostasis: From discovery to obesity therapy

Molecular metabolism (Germany), 2021-06, Vol.48, p.101206, Article 101206

2021

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Voluntary exercise prevents the obese and diabetic metabolic syndrome of the melanocortin-4 receptor knockout mouse

The FASEB journal, 2009-02, Vol.23 (2), p.642-655

2009

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The Proopiomelanocortin System

Annals of the New York Academy of Sciences, 1999-10, Vol.885 (1), p.1-21

1999

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Structure-activity relationship and metabolic stability studies of backbone cyclization and N-methylation of melanocortin peptides

Biopolymers, 2008, Vol.90 (5), p.671-682

2008

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The Parallel Structure-Activity Relationship Screening of Three Compounds Identifies the Common Agonist Pharmacophore of Pyrrolidine Bis-Cyclic Guanidine Melanocortin-3 Receptor (MC3R) Small-Molecule Ligands

International journal of molecular sciences, 2023-06, Vol.24 (12), p.10145

2023

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Structure–Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands

Molecules (Basel, Switzerland), 2019-04, Vol.24 (8), p.1463

2019

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α-MSH tripeptide analogs activate the melanocortin 1 receptor and reduce UV-induced DNA damage in human melanocytes

Pigment cell and melanoma research, 2009-10, Vol.22 (5), p.635-644

2009

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Implication of the melanocortin-3 receptor in the regulation of food intake

European journal of pharmacology, 2011-06, Vol.660 (1), p.80-87

2011

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Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor

Regulatory peptides, 2001-05, Vol.99 (1), p.1-7

2001

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Allosteric Modulators of Drug Targets

Journal of medicinal chemistry, 2019-01, Vol.62 (1), p.1-2

2019

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Backbone Cyclic Peptidomimetic Melanocortin-4 Receptor Agonist as a Novel Orally Administrated Drug Lead for Treating Obesity

Journal of medicinal chemistry, 2008-02, Vol.51 (4), p.1026-1034

2008

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The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: The melanocortin agonist paradigm

Bioorganic & medicinal chemistry, 2010-01, Vol.18 (2), p.580-589

2010

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Design of peptides, proteins, and peptidomimetics in chi space

Biopolymers, 1997, Vol.43 (3), p.219-266

1997

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Structure Activity Studies of the Melanocortin-4 Receptor by in Vitro Mutagenesis: Identification of Agouti-Related Protein (AGRP), Melanocortin Agonist and Synthetic Peptide Antagonist Interaction Determinants

Biochemistry (Easton), 2001-05, Vol.40 (20), p.6164-6179

2001

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Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors: Part 2 Modifications at the Phe Position

Journal of medicinal chemistry, 2002-07, Vol.45 (14), p.3073-3081

2002

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Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors. 1. Modifications at the His Position

Journal of medicinal chemistry, 2002-06, Vol.45 (13), p.2801-2810

2002

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Bone Morphogenetic Protein (BMP) Signaling Controls Hair Pigmentation by Means of Cross-Talk with the Melanocortin Receptor-1 Pathway

Proceedings of the National Academy of Sciences - PNAS, 2005-01, Vol.102 (1), p.93-98

2005

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Identification of Putative Agouti-Related Protein(87−132)-Melanocortin-4 Receptor Interactions by Homology Molecular Modeling and Validation Using Chimeric Peptide Ligands

Journal of medicinal chemistry, 2004-04, Vol.47 (9), p.2194-2207

2004

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Ghrelin-induced food intake and growth hormone secretion are altered in melanocortin 3 and 4 receptor knockout mice

Peptides (New York, N.Y. : 1980), 2005-10, Vol.26 (10), p.1720-1727

2005

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Molecular Basis for the Interaction of [Nle4,d-Phe7]Melanocyte Stimulating Hormone with the Human Melanocortin-1 Receptor (Melanocyte α-MSH Receptor)

The Journal of biological chemistry, 1997-09, Vol.272 (37), p.23000-23010

1997

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Characterization of Melanocortin NDP-MSH Agonist Peptide Fragments at the Mouse Central and Peripheral Melanocortin Receptors

Journal of medicinal chemistry, 2001-06, Vol.44 (13), p.2247-2252

2001

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Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors. 4. Modifications at the Trp Position

Journal of medicinal chemistry, 2002-12, Vol.45 (26), p.5736-5744

2002

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Progress in the development of melanocortin receptor selective ligands

Current pharmaceutical design, 2004-01, Vol.10 (28), p.3443-3479

2004

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Prevalence of pathogenetic MC4R mutations in Italian children with early onset obesity, tall stature and familial history of obesity

BMC medical genetics, 2009-03, Vol.10 (1), p.25-25, Article 25

2009

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Melanocortin ligands: 30 years of structure-activity relationship (SAR) studies

The melanocortin pathway and energy homeostasis: From discovery to obesity therapy

Voluntary exercise prevents the obese and diabetic metabolic syndrome of the melanocortin-4 receptor knockout mouse

The Proopiomelanocortin System

Structure-activity relationship and metabolic stability studies of backbone cyclization and N-methylation of melanocortin peptides

The Parallel Structure-Activity Relationship Screening of Three Compounds Identifies the Common Agonist Pharmacophore of Pyrrolidine Bis-Cyclic Guanidine Melanocortin-3 Receptor (MC3R) Small-Molecule Ligands

Structure–Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands

α-MSH tripeptide analogs activate the melanocortin 1 receptor and reduce UV-induced DNA damage in human melanocytes

Implication of the melanocortin-3 receptor in the regulation of food intake

Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor

Allosteric Modulators of Drug Targets

Backbone Cyclic Peptidomimetic Melanocortin-4 Receptor Agonist as a Novel Orally Administrated Drug Lead for Treating Obesity

The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: The melanocortin agonist paradigm

Design of peptides, proteins, and peptidomimetics in chi space

Structure Activity Studies of the Melanocortin-4 Receptor by in Vitro Mutagenesis: Identification of Agouti-Related Protein (AGRP), Melanocortin Agonist and Synthetic Peptide Antagonist Interaction Determinants

Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors: Part 2 Modifications at the Phe Position

Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors. 1. Modifications at the His Position

Bone Morphogenetic Protein (BMP) Signaling Controls Hair Pigmentation by Means of Cross-Talk with the Melanocortin Receptor-1 Pathway

Identification of Putative Agouti-Related Protein(87−132)-Melanocortin-4 Receptor Interactions by Homology Molecular Modeling and Validation Using Chimeric Peptide Ligands

Ghrelin-induced food intake and growth hormone secretion are altered in melanocortin 3 and 4 receptor knockout mice

Molecular Basis for the Interaction of [Nle4,d-Phe7]Melanocyte Stimulating Hormone with the Human Melanocortin-1 Receptor (Melanocyte α-MSH Receptor)

Characterization of Melanocortin NDP-MSH Agonist Peptide Fragments at the Mouse Central and Peripheral Melanocortin Receptors

Structure−Activity Relationships of the Melanocortin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH2 at the Mouse Melanocortin Receptors. 4. Modifications at the Trp Position

Progress in the development of melanocortin receptor selective ligands

Prevalence of pathogenetic MC4R mutations in Italian children with early onset obesity, tall stature and familial history of obesity

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