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Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. 2015

Alfonso Carotenuto, and Francesco Merlino, and Minying Cai, and Diego Brancaccio, and Ali Munaim Yousif, and Ettore Novellino, and Victor J Hruby, and Paolo Grieco
Dipartimento di Farmacia, Università di Napoli Federico II , Via D. Montesano, 49, 80131, Naples, Italy.

The melanocortin receptors 3 and 4 control energy homeostasis, food-intake behavior, and correlated pathophysiological conditions. The melanocortin-4 receptor (MC4R) has been broadly investigated. In contrast, the knowledge related to physiological roles of the melanocortin-3 receptor (MC3R) is lacking because of the limited number of known MC3R selective ligands. Here, we report the design, synthesis, biological activity, conformational analysis, and docking with receptors of two potent and selective agonists at the human MC3 receptor.

UI MeSH Term Description Entries
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D008968 Molecular Conformation The characteristic three-dimensional shape of a molecule. Molecular Configuration,3D Molecular Structure,Configuration, Molecular,Molecular Structure, Three Dimensional,Three Dimensional Molecular Structure,3D Molecular Structures,Configurations, Molecular,Conformation, Molecular,Conformations, Molecular,Molecular Configurations,Molecular Conformations,Molecular Structure, 3D,Molecular Structures, 3D,Structure, 3D Molecular,Structures, 3D Molecular
D009074 Melanocyte-Stimulating Hormones Peptides with the ability to stimulate pigmented cells MELANOCYTES in mammals and MELANOPHORES in lower vertebrates. By stimulating the synthesis and distribution of MELANIN in these pigmented cells, they increase coloration of skin and other tissue. MSHs, derived from pro-opiomelanocortin (POMC), are produced by MELANOTROPHS in the INTERMEDIATE LOBE OF PITUITARY; CORTICOTROPHS in the ANTERIOR LOBE OF PITUITARY, and the hypothalamic neurons in the ARCUATE NUCLEUS OF HYPOTHALAMUS. MSH,Melanocyte Stimulating Hormone,Melanocyte-Stimulating Hormone,Melanophore Stimulating Hormone,Melanotropin,MSH (Melanocyte-Stimulating Hormones),Melanophore-Stimulating Hormone,Hormone, Melanocyte Stimulating,Hormone, Melanocyte-Stimulating,Hormone, Melanophore Stimulating,Melanocyte Stimulating Hormones,Stimulating Hormone, Melanocyte,Stimulating Hormone, Melanophore
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000242 Cyclic AMP An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH. Adenosine Cyclic 3',5'-Monophosphate,Adenosine Cyclic 3,5 Monophosphate,Adenosine Cyclic Monophosphate,Adenosine Cyclic-3',5'-Monophosphate,Cyclic AMP, (R)-Isomer,Cyclic AMP, Disodium Salt,Cyclic AMP, Monoammonium Salt,Cyclic AMP, Monopotassium Salt,Cyclic AMP, Monosodium Salt,Cyclic AMP, Sodium Salt,3',5'-Monophosphate, Adenosine Cyclic,AMP, Cyclic,Adenosine Cyclic 3',5' Monophosphate,Cyclic 3',5'-Monophosphate, Adenosine,Cyclic Monophosphate, Adenosine,Cyclic-3',5'-Monophosphate, Adenosine,Monophosphate, Adenosine Cyclic
D000521 alpha-MSH A 13-amino acid peptide derived from proteolytic cleavage of ADRENOCORTICOTROPIC HORMONE, the N-terminal segment of ACTH. ACTH (1-13) is amidated at the C-terminal to form ACTH (1-13)NH2 which in turn is acetylated to form alpha-MSH in the secretory granules. Alpha-MSH stimulates the synthesis and distribution of MELANIN in MELANOCYTES in mammals and MELANOPHORES in lower vertebrates. MSH, alpha,alpha Intermedin,alpha-Melanocyte-Stimulating Hormone,(Des-Acetyl)-alpha-MSH,(Desacetyl)alpha-MSH,ACTH (1-13),ACTH (1-13)NH2,ACTH(1-13),Acetylated ACTH (1-13)NH2,Adrenocorticotropin (1-13)NH2,DE-alpha-MSH,Des-Acetyl MSH,Desacetyl alpha-MSH,Desacetyl alpha-Melanocyte-Stimulating Hormone,MSH, (Desacetyl)alpha-,alpha-Melanotropin,Desacetyl alpha MSH,Desacetyl alpha Melanocyte Stimulating Hormone,Hormone, Desacetyl alpha-Melanocyte-Stimulating,Hormone, alpha-Melanocyte-Stimulating,Intermedin, alpha,MSH, Des-Acetyl,alpha MSH,alpha Melanocyte Stimulating Hormone,alpha Melanotropin,alpha-MSH, Desacetyl,alpha-Melanocyte-Stimulating Hormone, Desacetyl
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D044101 Receptors, Melanocortin A family of G-protein-coupled receptors that have specificity for MELANOCYTE-STIMULATING HORMONES and ADRENOCORTICOTROPIC HORMONE. There are several subtypes of melanocortin receptors, each having a distinct ligand specificity profile and tissue localization. Melanocortin Receptors,Melanocortin Receptor,Receptor, Melanocortin
D044102 Receptor, Melanocortin, Type 1 A melanocortin receptor subtype found primarily in MELANOCYTES. It shows specificity for ALPHA-MSH and ADRENOCORTICOTROPIC HORMONE. Loss of function mutations of the type 1 melanocortin receptor account for the majority of red hair and fair skin recessive traits in human. Melanocortin Receptor 1,MC1 Receptor,Melanocortin-1 Receptor,Melanocyte Melanocortin Receptor,Receptor, Melanocortin-1,Melanocortin 1 Receptor,Melanocortin Receptor, Melanocyte,Receptor 1, Melanocortin,Receptor, MC1,Receptor, Melanocortin 1,Receptor, Melanocyte Melanocortin

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