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

Regulatory Peptides

Volumn 99, Issue 1, 2001, Pages 1-7

  Haskell Luevano, Carrie ^a   Monck, Eileen K ^a  

^a UNIVERSITY OF FLORIDA   (United States)

Author keywords

Energy Homeostasis; Feeding; MC4R; Melanotropin; Neuropeptide; Obesity

Indexed keywords

ACETYLNORLEUCYLASPARTYL DEXTRO PHENYLALANYLARGINYLTRYPTOPHYLLYSINE; ACETYLSERYLTYROSYLSERYLNORLEUCYLGLUTAMYLHISTIDYL DEXTRO PHENYLALANYLARGINYLTRYPTOPHYLGLYCYLLYSYLPROLYLVALINE; AGOUTI RELATED PROTEIN; ALPHA INTERMEDIN; BETA GALACTOSIDASE; COMPLEMENTARY DNA; G PROTEIN COUPLED RECEPTOR; MELANOCORTIN; MELANOCORTIN 3 RECEPTOR; MELANOCORTIN 4 RECEPTOR; MUTANT PROTEIN; N ACETYL ALPHA INTERMEDIN[4-10]CYCLO[4 NORLEUCINE 5 ASPARTIC ACID 7 [3 (2 NAPHTHYL)ALANINE] 10 LYSINAMIDE]; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; ENZYME ACTIVITY; FEEDING BEHAVIOR; FIBROBLAST; FOOD INTAKE; HUMAN; HUMAN CELL; KIDNEY CELL; METABOLIC BALANCE; NONHUMAN; OBESITY; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; TRANSGENIC MOUSE;

ANIMALS; BRAIN; CELL LINE; HUMANS; MICE; PEPTIDE FRAGMENTS; RECEPTOR, MELANOCORTIN, TYPE 4; RECEPTORS, PEPTIDE;

AGOUTI; MUS MUSCULUS;

EID: 0035810771     PISSN: 01670115     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0167-0115(01)00234-8     Document Type: Article

References (44)

1. Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor
2. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein
3. The mouse mahogany locus encodes a transmembrane form of human attractin
4. The mahogany protein is a receptor involved in suppression of obesity
5. Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA
6. The cloning of a family of genes that encode the melanocortin receptors
7. Identification of a receptor for g melanotropin and other proopiomelanocortin peptides in the hypothalamus and limbic system
8. Localization of the melanocortin-4 receptor (MC4-R) in neuroendocrine and autonomic control circuits in the brain
9. Molecular cloning of a novel melanocortin receptor
10. Molecular cloning, expression, and gene localization of a fourth melanocortin receptor
11. Molecular cloning, expression, and characterization of a fifth melanocortin receptor
12. Molecular characterization of the mouse agouti locus
13. Cloning of the mouse agouti gene predicts a secreted protein ubiquitously expressed in mice carrying the lethal yellow mutation
14. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
15. Targeted disruption of the melanocortin-4 receptor results in obesity in mice
16. Characterization of agouti-related protein binding to melanocortin receptors
17. Overexpression of AGRT leads to obesity in transgenic mice
18. Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass
19. Severe early-onset obesity, adrenal insufficiency and red hair pigmentation caused by POMC mutations in humans
20. Frameshift mutation in human MC4R is associated with a dominant form of obesity
21. Frameshift mutation in MC4R associated with dominantly inherited human obesity
22. Several mutations in the melanocortin-4 receptor gene including a nonsense and a frameshift mutation associated with dominantly inherited obesity in humans
23. A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse
24. Hypothalamic expression of ART, a novel gene related to agouti, is up-regulated in obese and diabetic mutant mice
25. Characterization of the neuroanatomical distribution of agouti related protein (AGRP) immunoreactivity in the rhesus monkey and the rat
26. The neuropeptide Y/agouti gene-related protein (AGRP) brain circuitry in normal, anorectic, and monosodium glutamate-treated mice
27. Integration of NPY, AGRP, and melanocortin signals in the hypothalamic paraventricular nucleus: Evidence of a cellular basis for the adipostat
28. Coexpression of AGRP and NPY in fasting-activated hypothalamic neurons
29. Altered expression of agouti related protein (AGRP) and its colocalization with neuropeptide and (NPY) in the arcuate nucleus of the hypothalamus during lactation
30. Effects of neuropeptide Y deficiency on hypothalamic agouti-related protein expression and responsiveness to melanocortin analogues
31. Sensitivity to leptin and susceptibility to seizures of mice lacking neuropeptide Y
32. Potent and prolonged acting cyclic lactam analogues of a-melanotropin: Design based on molecular dynamics
33. Long-term orexigenic effects of AgRP-(83-132) involve mechanisms other than melanocortin receptor blockade
34. A colorimetric assay for measuring activation of Gs- and Gq-coupled signaling pathways
35. A ligand-mimetic model for constitutive activation of the melanocortin-1 receptor
36. pA, a new scale for the measurement of drug antagonism
37. 2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors
38. Structure activity studies of the melanocortin antagonist SHU9119 modified at the 6, 7, 8, and 9 positions
39. Neuropeptide Y and human pancreatic polypeptide stimulate feeding behavior in rats
40. Neuropeptide Y injected in the paraventricular hypothalamus: A powerful stimullant of feeding behavior
41. A receptor subtype involved in neuropeptide-Y-induced food intake
42. Anatomy of an endogenous antagonist: Relationship between Agouti-related protein and proopiomelanocortin in brain
43. Switching agonist-antagonist properties of opiate alkaloids at the delta opioid receptor using mutations based on the structure of the orphanin FQ receptor
44. AGRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor