Molecular determination of agouti-related protein binding to human melanocortin-4 receptor

Molecular Pharmacology

Volumn 64, Issue 1, 2003, Pages 94-103

  Yang, Yingkui ^a   Chen, Min ^b   Lai, Yumei ^b   Gantz, Ira ^b   Yagmurlu, Aydin ^a   Georgeson, Keith E ^a   Harmon, Carroll M ^a  

^a Kentucky   (United States)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AGOUTI PROTEIN; AGOUTI RELATED PROTEIN; AGOUTI RELATED PROTEIN 110-117; AGOUTI RELATED PROTEIN 87-132; MELANOCORTIN 1 RECEPTOR; MELANOCORTIN 4 RECEPTOR; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ARTICLE; BINDING AFFINITY; BINDING SITE; CHIMERA; FEEDING BEHAVIOR; HUMAN; HUMAN CELL; HYPOTHALAMUS; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN PROTEIN INTERACTION;

ALPHA-MSH; AMINO ACID SEQUENCE; ANIMALS; CELLS, CULTURED; CYCLIC AMP; HUMANS; INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS; IODINE RADIOISOTOPES; MELANOCYTE-STIMULATING HORMONES; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; PEPTIDE FRAGMENTS; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN FOLDING; PROTEINS; RECEPTOR, MELANOCORTIN, TYPE 4; RECEPTORS, CORTICOTROPIN; RECOMBINANT FUSION PROTEINS; SEQUENCE ALIGNMENT; TRANSFECTION;

EID: 0038237053     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.64.1.94     Document Type: Article

References (30)

1. Bagnol D, Lu XY, Kaelin CB, Day HE, Ollmann M, Gantz I, Akil H, Barsh GS, and Watson SJ (1999) Anatomy of an endogenous antagonist: relationship between Agouti-related protein and proopiomelanocortin in brain. J Neurosci 19:RC26.
2. Baldwin JM (1993) The probable arrangement of the helices in G protein-coupled receptors. EMBO (Eur Mol Biol Organ) J 12:1693-1703.
3. Barsh GS, Ollmann MM, Wilson BD, Miller KA, and Gunn TM (1999) Molecular pharmacology of Agouti protein in vitro and in vivo. Ann NY Acad Sci 885:143-152.
4. Bolin KA, Anderson DJ, Trulson JA, Thompson DA, Wilken J, Kent SB, Gantz I, and Millhauser GL (1999) NMR structure of a minimized human agouti related protein prepared by total chemical synthesis. FEBS Lett 451:125-131.
5. Casarosa P, Menge WM, Minisini R, Otto C, Heteren J, Jongejan A, Timmerman H, Moepps B, Kirchhoff F, Mertens T, et al. (2003) Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor. J Biol Chem 278:5172-5178.
6. Dinulescu DM and Cone RD (2000) Agouti and Agouti-related protein: Analogies and contrasts. J Biol Chem 275:6695-6698.
7. Fan W, Boston BA, Kesterson RA, Hruby VJ, and Cone RD (1997) Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature (Lond) 385:165-168.
8. Gantz I, Miwa H, Konda Y, Shimoto Y, Tashiro T, Watson SJ, DelValle J, and Yamada T (1993) Molecular cloning, expression and gene localization of a fourth melanocortin receptor. J Biol Chem 268:15174-15179.
9. Hahn TM, Breininger JF, Baskin DG, and Schwartz MW (1998) Coexpression of AGRP and NPY in fasting-activated hypothalamic neurons. Nat Neurosci 1:271-272.
10. Haskell-Luevano C and Monck EK (2001) Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor. Regul Pept 99:1-7.
11. Haskell-Luevano C, Sawyer TK, Trumpp-Kallmeyer S, Bikker J, Humblet C, Gantz I, and Hruby VJ (1996) Three-dimensional molecular models of the hMC1R melanocortin receptor: complexes with melanotropin peptide agonists. Drug Des Discov 14:197-211.
12. 2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J Med Chem 38:3454-3461.
13. Huszar D, Lynch CA, Fairchild-Huntress V, Dunmore JH, Fang Q, Berkemeier LR, Gu W, Kesterson RA, Boston BA, Cone RD, et al. (1997) Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell 88:131-141.
14. Ji TH, Grossmann M, and Ji I (1998) G protein-coupled receptors. J Biol Chem 273:17299-17302.
15. Joubert L, Claeysen S, Sebben M, Bessis AS, Clark RD, Martin RS, Bockaert J, and Dumuis A (2002) A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists. J Biol Chem 277:25502-25511.
16. MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ, et al. (2002) The role of melanocortins in body weight regulation: opportunities for the treatment of obesity. Eur J Pharmacol 450:93-109.
17. McNulty JC, Thompson DA, Bolin KA, Wilken J, Barsh GS, and Millhauser GL (2001) High-resolution NMR structure of the chemically-synthesized melanocortin receptor binding domain AGRP(87-132) of the agouti-related protein. Biochemistry 40:15520-15527.
18. Mizuno TM, Kleopoulos SP, Bergen HT, Roberts JL, and Priest CA (1998) Hypothalamic pro-opiomelanocortin mRNA is reduced by fasting and corrected in ob/ob and db/db mice, but is stimulated by leptin. Diabetes 47:294-297.
19. Mountjoy KG, Robbins LS, Mortrud MT, and Cone RD (1992) The cloning of a family of genes that encode the melanocortin receptors. Science (Wash DC) 257:1248-1251.
20. Nijenhuis WAJ, Oosterom J, and Adan RAH (2001) AGRP (83-132) acts as an inverse agonist on the human melanocortin-4 receptor. Mol Endocrinol 15:164-171.
21. Ollmann MM, Wilson BD, Yang Y-K, Kerns JA, Chen Y, Gantz I, and Barsh GS (1997) Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science (Wash DC) 278:135-138.
22. Strange PG (2002) Mechanisms of inverse agonism at G-protein-coupled receptors. Trends Pharmacol Sci 23:89-95.
23. Tota MR, Smith TS, Mao C, MacNeil T, Mosley RT, Van der Ploeg LH, and Fong TM (1999) Molecular interaction of agouti protein and agouti-related protein with human melanocortin receptors. Biochemistry 38:897-904.
24. Wilson BD, Ollmann MM, and Barsh GS (1999) The role of agouti-related protein in regulating body weight. Mol Med Today 5:250-256.
25. Yang Y-K, Dickinson C, Haskell-Leuvano C, and Gantz I (1997a) Molecular Basis for the interaction of melanocortin peptides with the human melanocortin-1 Receptor (α-MSH receptor). J Biol Chem 272:23000-23010.
26. Yang Y-K, Ollmann MM, Barsh GS, Yamada T, and Gantz I (1997b) Effects of Recombinant agouti signaling protein on melanocortin action at the human melanocortin receptors. Mol Endocrinol 11:274-280.
27. Yang Y-K, Dickinson C, Kent SB, and Gantz I (1999a) Characterization of AGRP binding to the melanocortin receptors. Mol Endocrinol 13:148-155.
28. Yang Y-K, Dickinson C, Zeng Q, Li JY, and Gantz I (1999b) Contribution of melanocortin receptor exoloops to agouti-related protein binding. J Biol Chem 274:14100-14106.
29. Yang Y-K, Fong T, Dickinson C, Kent SB, Ploeg VD Lex HT, and Gantz I (2000) Molecular determinants of ligand binding to the human melanocortin-4 receptor. Biochemistry 39:14900-14911.
30. Yang Y-K, Dickinson C, Lai YM, Li JY, and Gantz I (2001) Functional properties of an agouti signaling protein variant and characteristics of its cognate radioligand. Am J Physiol 281:R1877-R18786.