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

Volumn 45, Issue 14, 2002, Pages 3073-3081

  Holder, Jerry Ryan ^a   Bauzo, Rayna M ^a   Xiang, Zhimin ^a   Haskell Luevano, Carrie ^a  

^a UNIVERSITY OF FLORIDA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLHISTIDINE DEXTRO PHENYLALANYLARGINYLTRYPTOPHANYLAMINE; AGOUTI RELATED PROTEIN; ALPHA INTERMEDIN; MELANOCORTIN; MELANOCORTIN 1 RECEPTOR; MELANOCORTIN 3 RECEPTOR; MELANOCORTIN 4 RECEPTOR; MELANOCORTIN 5 RECEPTOR; MELANOCORTIN RECEPTOR; N ACETYL ALPHA INTERMEDIN[4-10]CYCLO[4 NORLEUCINE 5 ASPARTIC ACID 7 [3 (2 NAPHTHYL)ALANINE] 10 LYSINAMIDE]; PEPTIDE LIBRARY; PHENYLALANINE; TETRAPEPTIDE; UNCLASSIFIED DRUG;

AGONIST; AMINO ACID SEQUENCE; ARTICLE; CHIRALITY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG POTENCY; EMBRYO; ENERGY METABOLISM; FOOD INTAKE; HORMONE RECEPTOR INTERACTION; HUMAN; HUMAN CELL; KNOCKOUT GENE; MOUSE; NONHUMAN; PRIMATE; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

AMINO ACID SUBSTITUTION; ANIMALS; CELL LINE; HUMANS; MICE; OLIGOPEPTIDES; PHENYLALANINE; RECEPTOR, MELANOCORTIN, TYPE 3; RECEPTOR, MELANOCORTIN, TYPE 4; RECEPTORS, CORTICOTROPIN; RECEPTORS, MELANOCORTIN; RECEPTORS, PEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037019281     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010524p     Document Type: Article

References (44)

1. The melanocortin receptors: Agonists, antagonists, and the hormonal control of pigmentation
2. α-melanotropin: The minimal active sequence in the frog skin bioassay
3. α-melanotropin: The minimal active sequence in the lizard skin bioassay
4. Truncation studies of α-melanotropin peptides identifies tripeptide analogues exhibiting prolonged agonist bioactivity
5. Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor
6. Hypothalamic expression of ART, a novel gene related to agouti, is up-regulated in obese and diabetic mutant mice
7. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
8. Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass
9. A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse
10. Targeted disruption of the melanocortin-4 receptor results in obesity in mice
11. Melanotropins: Structural, conformational and biological considerations in the development of superpotent and super-prolonged analogues
12. The cloning of a family of genes that encode the melanocortin receptors
13. A ligand-mimetic model for constitutive activation of the melanocortin-1 receptor
14. Exocrine gland dysfunction in MC5-R deficient mice: Evidence for coordinated regulation of exocrine gland functions by melanocortin peptides
15. 2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors
16. 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
17. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
18. Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): Evaluation in vitro and in vivo
19. Evidence that orexigenic effects of melanocortin 4 receptor antagonist HS014 are mediated by neuropeptide Y
20. Long-term orexigenic effect of a novel melanocortin 4 receptor selective antagonist
21. Selective, high affinity peptide antagonists of a-melanotropin action at human melanocortin receptor 4: Their synthesis and biological evaluation in vitro
22. Structure activity studies of the melanocortin antagonist SHU9119 modified at the 6, 7, 8, and 9 positions
23. A novel selective melaocortin-4 receptor agonist reduces food intake in rats and mice without producing aversive consequences
24. Three-dimensional molecular models of the hMC1R melanocortin receptor: Complexes with melanotropin peptide agonists
25. 7] melanocyte stimulating hormone with the human melanocortin-1 receptor (melanocyte α-MSH receptor)
26. Molecular determinants of ligand binding to the human melanocortin-4 receptor
27. In vitro mutagenesis studies of melanocortin receptor coupling and ligand binding
28. Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors
29. Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA
30. Identification of a receptor for γ melanotropin and other proopiomelanocortin peptides in the hypothalamus and limbic system
31. Molecular cloning of a novel melanocortin receptor
32. Analogues of lactam derivatives of α-melanotropin with basic and acidic residues
33. Structure-function studies on the cyclic peptide MT-II, lactam derivative of α-melanotropin
34. Rapid communication: A novel melanocortin 4 receptor (MC4R) gene mutation associated with morbid obesity
35. A frameshift mutation in human MC4R is associated with a dominant form of obesity
36. Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity
37. Dominant and recessive inheritance of morbid obesity associated with melanocortin 4 receptor deficiency
38. Phenotypes in three pedigrees with autosomal dominant obesity caused by haploinsufficiency mutations in the melanocortin-4 receptor gene
39. Several mutations in the melanocortin-4 receptor gene including a nonsense and a frameshift mutation associated with dominantly inherited obesity in humans
40. Molecular cloning, expression, and characterization of a fifth melanocortin receptor
41. Color test for detection of free terminal amino groups in the solid-phase synthesis of peptides
42. Colorimetric assay for measuring activation of Gs- and Gq-coupled signaling pathways
43. pA, a new scale for the measurement of drug antagonism