Molecular basis of melanocortin-4 receptor for AGRP inverse agonism

Regulatory Peptides

Volumn 136, Issue 1-3, 2006, Pages 40-49

  Chen, Min ^a   Celik, Ahmet ^a   Georgeson, Keith E ^a   Harmon, Carroll M ^a   Yang, Yingkui ^a  

^a Kentucky   (United States)

Author keywords

AGRP; GPCR; Inverse agonist; MC4R; Obesity

Indexed keywords

AGOUTI RELATED PROTEIN; CHIMERIC PROTEIN; CYCLIC AMP; MELANOCORTIN 1 RECEPTOR; MELANOCORTIN 4 RECEPTOR; MEMBRANE PROTEIN;

AGONIST; AMINO TERMINAL SEQUENCE; ARTICLE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; DNA TEMPLATE; GENE MUTATION; HUMAN; HUMAN CELL; MOLECULAR DYNAMICS; MOLECULAR MECHANICS; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN STRUCTURE;

AGOUTI-RELATED PROTEIN; AMINO ACID SEQUENCE; CYCLIC AMP; HUMANS; INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS; LIGANDS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; OBESITY; PROTEIN BINDING; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, MELANOCORTIN, TYPE 4; RECOMBINANT FUSION PROTEINS; TRANSFECTION;

AGOUTI;

EID: 33747366626     PISSN: 01670115     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.regpep.2006.04.010     Document Type: Article

References (42)

1. Huszar D., Lynch C.A., Fairchild-Huntress V., Dunmore J.H., Fang Q., Berkemeier L.R., Gu W., Kesterson R.A., Boston B.A., Cone R.D., et al. Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell 88 1 (1997) 131-141
2. Von Frijtag J.C., Croiset G., Gispen W.H., Adan R.A., and Wiegant V.M. The role of central melanocortin receptors in the activation of the hypothalamus-pituitary-adrenal-axis and the induction of excessive grooming. Br J Pharmacol 123 8 (1998) 1503-1508
3. Ebihara K., Ogawa Y., Katsuura G., Numata Y., Masuzaki H., Satoh N., Tamaki M., Yoshioka T., Hayase M., Matsuoka N., et al. Involvement of agouti-related protein, an endogenous antagonist of hypothalamic melanocortin receptor, in leptin action. Diabetes 48 10 (1999) 2028-2033
4. Ollmann M.M., Wilson B.D., Yang Y.K., Kerns J.A., Chen Y., Gantz I., and Barsh G.S. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science 278 5335 (1997) 135-138
5. Chen G., Way J., Armour S., Watson C., Queen K., Jayawickreme C.K., Chen W.J., and Kenakin T. Use of constitutive G protein-coupled receptor activity for drug discovery. Mol Pharmacol 57 1 (2000) 125-134
6. Wade S.M., Lan K., Moore D.J., and Neubig R.R. Inverse agonist activity at the alpha(2A)-adrenergic receptor. Mol Pharmacol 59 3 (2001) 532-542
7. Lubrano-Berthelier C., Cavazos M., Dubern B., Shapiro A., Stunff C.L., Zhang S., Picart F., Govaerts C., Froguel P., Bougneres P., et al. Molecular genetics of human obesity-associated MC4R mutations. Ann N Y Acad Sci 994 (2003) 49-57
8. Farooqi I.S., Keogh J.M., Yeo G.S., Lank E.J., Cheetham T., and O'Rahilly S. Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene. N Engl J Med 348 12 (2003) 1085-1095
9. Farooqi I.S., Yeo G.S., Keogh J.M., Aminian S., Jebb S.A., Butler G., Cheetham T., and O'Rahilly S. Dominant and recessive inheritance of morbid obesity associated with melanocortin 4 receptor deficiency. J Clin Invest 106 2 (2000) 271-279
10. List J.F., and Habener J.F. Defective melanocortin 4 receptors in hyperphagia and morbid obesity. N Engl J Med 348 12 (2003) 1160-1163
11. Vaisse C., Clement K., Guy-Grand B., and Froguel P. A frameshift mutation in human MC4R is associated with a dominant form of obesity. Nat Genet 20 2 (1998) 113-114
12. Vaisse C., Clement K., Durand E., Hercberg S., Guy-Grand B., and Froguel P. Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity. J Clin Invest 106 2 (2000) 253-262
13. Srinivasan S., Lubrano-Berthelier C., Govaerts C., Picard F., Santiago P., Conklin B.R., and Vaisse C. Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans. J Clin Invest 114 8 (2004) 1158-1164
14. Yang Y.K., Dickinson C.J., Zeng Q., Li J.Y., Thompson D.A., and Gantz I. Contribution of melanocortin receptor exoloops to Agouti-related protein binding. J Biol Chem 274 20 (1999) 14100-14106
15. Tritos N.A., and Maratos-Flier E. Two important systems in energy homeostasis: melanocortins and melanin-concentrating hormone. Neuropeptides 33 5 (1999) 339-349
16. Guan X.M., Kobilka T.S., and Kobilka B.K. Enhancement of membrane insertion and function in a type IIIb membrane protein following introduction of a cleavable signal peptide. J Biol Chem 267 31 (1992) 21995-21998
17. Yang Y., Dickinson C., Haskell-Luevano C., and Gantz I. Molecular basis for the interaction of [Nle4,D-Phe7]melanocyte stimulating hormone with the human melanocortin-1 receptor. J Biol Chem 272 37 (1997) 23000-23010
18. Yang Y., Chen M., Lai Y., Gantz I., Yagmurlu A., Georgeson K.E., and Harmon C.M. Molecular determination of agouti-related protein binding to human melanocortin-4 receptor. Mol Pharmacol 64 1 (2003) 94-103
19. Yang Y.K., Fong T.M., Dickinson C.J., Mao C., Li J.Y., Tota M.R., Mosley R., Van Der Ploeg L.H., and Gantz I. Molecular determinants of ligand binding to the human melanocortin-4 receptor. Biochemistry 39 48 (2000) 14900-14911
20. Yang Y., Chen M., Lai Y., Gantz I., Georgeson K.E., and Harmon C.M. Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activity. J Biol Chem 277 23 (2002) 20328-20335
21. Tao Y.X. Molecular mechanisms of the neural melanocortin receptor dysfunction in severe early onset obesity. Mol Cell Endocrinol 239 1-2 (2005) 1-14
22. Yang Y., Chen M., Loux T.J., Georgeson K.E., and Harmon C.M. Molecular mechanism of the intracellular segments of the melanocortin-4 receptor for NDP-MSH signaling. Biochemistry 44 18 (2005) 6971-6979
23. Leurs R., Smit M.J., Alewijnse A.E., and Timmerman H. Agonist-independent regulation of constitutively active G-protein-coupled receptors. Trends Biochem Sci 23 11 (1998) 418-422
24. Wieland K., Bongers G., Yamamoto Y., Hashimoto T., Yamatodani A., Menge W.M., Timmerman H., Lovenberg T.W., and Leurs R. Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. J Pharmacol Exp Ther 299 3 (2001) 908-914
25. Casarosa P., Bakker R.A., Verzijl D., Navis M., Timmerman H., Leurs R., and Smit M.J. Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28. J Biol Chem 276 2 (2001) 1133-1137
26. Strange P.G. Mechanisms of inverse agonism at G-protein-coupled receptors. Trends Pharmacol Sci 23 2 (2002) 89-95
27. de Ligt R.A., Kourounakis A.P., and AP IJ. Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery. Br J Pharmacol 130 1 (2000) 1-12
28. Kenakin T. Inverse, protean, and ligand-selective agonism: matters of receptor conformation. FASEB J 15 3 (2001) 598-611
29. Samama P., Pei G., Costa T., Cotecchia S., and Lefkowitz R.J. Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor. Mol Pharmacol 45 3 (1994) 390-394
30. Lattion A., Abuin L., Nenniger-Tosato M., and Cotecchia S. Constitutively active mutants of the beta1-adrenergic receptor. FEBS Lett 457 3 (1999) 302-306
31. Smit M.J., Leurs R., Alewijnse A.E., Blauw J., Van Nieuw Amerongen G.P., Van De Vrede Y., Roovers E., and Timmerman H. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A 93 13 (1996) 6802-6807
32. Claeysen S., Sebben M., Becamel C., Eglen R.M., Clark R.D., Bockaert J., and Dumuis A. Pharmacological properties of 5-Hydroxytryptamine(4) receptor antagonists on constitutively active wild-type and mutated receptors. Mol Pharmacol 58 1 (2000) 136-144
33. Bakker R.A., Wieland K., Timmerman H., and Leurs R. Constitutive activity of the histamine H(1) receptor reveals inverse agonism of histamine H(1) receptor antagonists. Eur J Pharmacol 387 1 (2000) R5-R7
34. Alewijnse A.E., Smit M.J., Hoffmann M., Verzijl D., Timmerman H., and Leurs R. Constitutive activity and structural instability of the wild-type human H2 receptor. J Neurochem 71 2 (1998) 799-807
35. Nagaraja S., Iyer S., Liu X., Eichberg J., and Bond R.A. Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic beta2-adrenoceptor activation. Br J Pharmacol 127 5 (1999) 1099-1104
36. Schipani E., Langman C.B., Parfitt A.M., Jensen G.S., Kikuchi S., Kooh S.W., Cole W.G., and Juppner H. Constitutively activated receptors for parathyroid hormone and parathyroid hormone-related peptide in Jansen's metaphyseal chondrodysplasia. N Engl J Med 335 10 (1996) 708-714
37. Ellacott K.L., and Cone R.D. The central melanocortin system and the integration of short- and long-term regulators of energy homeostasis. Recent Prog Horm Res 59 (2004) 395-408
38. Chai B.X., Neubig R.R., Millhauser G.L., Thompson D.A., Jackson P.J., Barsh G.S., Dickinson C.J., Li J.Y., Lai Y.M., and Gantz I. Inverse agonist activity of agouti and agouti-related protein. Peptides 24 4 (2003) 603-609
39. Haskell-Luevano C., and Monck E.K. Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor. Regul Pept 99 1 (2001) 1-7
40. Nijenhuis W.A., Oosterom J., and Adan R.A. AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. Mol Endocrinol 15 1 (2001) 164-171
41. Gantz I., Miwa H., Konda Y., Shimoto Y., Tashiro T., Watson S.J., DelValle J., and Yamada T. Molecular cloning, expression, and gene localization of a fourth melanocortin receptor. J Biol Chem 268 20 (1993) 15174-15179
42. Bolin K.A., Anderson D.J., Trulson J.A., Thompson D.A., Wilken J., Kent S.B., Gantz I., and Millhauser G.L. NMR structure of a minimized human agouti related protein prepared by total chemical synthesis. FEBS Lett 451 2 (1999) 125-131