Molecular determinants of melanocortin 4 receptor ligand binding and MC4/MC3 receptor selectivity

Journal of Pharmacology and Experimental Therapeutics

Volumn 304, Issue 3, 2003, Pages 1217-1227

  Nickolls, Sarah A ^a,b   Cismowski, Mary I ^a   Wang, Xiaochuan ^a   Wolff, Meira ^a   Conlon, Paul J ^a   Maki, Richard A ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

^b NONE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; ASPARTIC ACID; ISOLEUCINE; MELANOCORTIN 3 RECEPTOR; MELANOCORTIN 4 RECEPTOR; PHENYLALANINE;

AMINO ACID SUBSTITUTION; ARTICLE; BINDING AFFINITY; HUMAN; HUMAN CELL; HYDROPHOBICITY; LIGAND BINDING; MOLECULAR INTERACTION; MOLECULAR MODEL; MOLECULAR RECOGNITION; MUTATION; OBESITY; PRIORITY JOURNAL; PROTEIN TERTIARY STRUCTURE; RECEPTOR BINDING; RECEPTOR SENSITIVITY;

AMINO ACID SEQUENCE; CELLS, CULTURED; CYCLIC AMP; HUMANS; HYDROPHOBICITY; LIGANDS; MEMBRANE PROTEINS; MOLECULAR SEQUENCE DATA; MUTAGENESIS; RECEPTOR, MELANOCORTIN, TYPE 3; RECEPTOR, MELANOCORTIN, TYPE 4; RECEPTORS, CORTICOTROPIN; TRANSFECTION;

EID: 0037371579     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.044974     Document Type: Article

References (30)

1. Bednarek MA, MacNeil T, Kalyani RN, Tang R, Van der Ploeg LH, and Weinberg DN (1999) Analogs of MTII, lactam derivatives of alpha-melanotropin, modified at the N-terminus and their selectivity at human melanocortin receptors 3, 4 and 5. Biochem Biophys Res Commun 261:209-213.
2. Bednarek MA, MacNeil T, Kalyani RN, Tang R, Van der Ploeg LH, and Weinberg DN (2001) Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro. J Med Chem 44:3665-3672.
3. Butler AA, Kesterson RA, Khong K, Cullen MJ, Pelleymounter MA, Dekoning J, Baetscher M, and Cone RD (2000) A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse. Endocrinology 141:3518-3521.
4. Butler AA, Marks DL, Fan W, Kuhn CM, Bartolome M, and Cone RD (2001) Melanocortin-4 receptor is required for acute homeostatic responses to increased dietary fat. Nat Neurosci 4:605-611.
5. Chen AS, Marsh DJ, Trumbauer ME, Frazier EG, Guan XM, Yu H, Rosenblum CI, Vongs A, Feng Y, Cao L, et al. (2000) Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass. Nat Genet 26:97-102.
6. 50) of an enzymic reaction. Biochem Pharmacol 55:3099-3108.
7. Cordeaux Y, Nickolls SA, Flood LA, Graber SG, and Strange PG (2001) Agonist regulation of D(2) dopamine receptor/G protein interaction. Evidence for agonist selection of G protein subtype. J Biol Chem 276:28667-28675.
8. Covic L, Gresser AL, Talavera J, Swift S, and Kuliopulos A (2002) Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides. Proc Natl Acad Sci USA 99:643-648.
9. De Lean A, Stadel JM, and Lefkowitz RJ (1980) A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J Biol Chem 255:7108-7117.
10. 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.
11. Gilman AG (1987) G proteins: transducers of receptor-generated signals. Annu Rev Biochem 56:615-649.
12. Gu W, Tu Z, Kleyn PW, Kissebah A, Duprat L, Lee J, Chin W, Maruti S, Deng N, Fisher SL, et al. (1999) Identification and functional analysis of novel human melanocortin-4 receptor variants. Diabetes 48:635-639.
13. Haskell-Luevano C, Cone RD, Monck EK, and Wan YP (2001) 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. Biochemistry 40:6164-6179.
14. Haskell-Luevano C, Hendrata S, North C, Sawyer TK, Hadley ME, Hruby VJ, Dickinson C, and Gantz I (1997) Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. J Med Chem 40:2133-2139.
15. 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.
16. 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.
17. Lu D, Willard D, Patel IR, Kadwell S, Overton L, Kost T, Luther M, Chen R, Woychik WR, Wilkison WO, et al. (1994) Agouti protein is an antagonist of the melanocyte-stimulating-hormone receptor. Nature (Lond) 371:799-802.
18. 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.
19. Nijenhuis WA, Oosterom J, and Adan RA (2001) AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. Mol Endocrinol 15:164-171.
20. Ollmann MM, Wilson BD, Yang YK, 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.
21. Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, et al. (2001) Crystal structure of rhodopsin: a G protein coupled receptor. Science (Wash DC) 289:739-745.
22. Sahm UG, Olivier GW, Branch SK, Moss SH, and Pouton CW (1994) Synthesis and biological evaluation of alpha-MSH analogues substituted with alanine. Peptides 15:1297-1302.
23. Samama P, Cotecchia S, Costa T, and Lefkowitz RJ (1993) A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model. J Biol Chem 268:4625-4636.
24. Siehler S, Seuwen K, and Hoyer D (1999) Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn-Schmiedeberg's Arch Pharmacol 360:488-499.
25. Strange PG (1999) G protein coupled receptors, conformations and states. Biochem Pharmacol 58:1081-1088.
26. Van der Ploeg LHT, Martin WJ, Howard AD, Nargund RP, Austin CP, Guan X, Drisko J, Cashen D, Sebhat I, Patchett AA, et al. (2002) A role for the melanocortin 4 receptor in sexual function. Proc Nat Acad Sci USA 99:11381-11386.
27. Yang Y, Chen M. Lai Y, Gantz I, Georgeson KE, and Harmon CM (2002) Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activity. J Biol Chem 277:20328-20335.
28. Yang Y, Dickinson C, Haskell-Luevano C, and Gantz I (1997) Molecular basis for the interaction of [Nle4, D-Phe7]melanocyte stimulating hormone with the human melanocortin-1 receptor. J Biol Chem 272:23000-23010.
29. Yang YK, Fong TM, Dickinson CJ, Mao C, Li JY, Tota MR, Mosley R, Van Der Ploeg LH, and Gantz I (2000) Molecular determinants of ligand binding to the human melanocortin-4 receptor. Biochemistry 39:14900-14911.
30. Yang YK, Thompson DA, Dickinson CJ, Wilken J, Barsh GS, Kent SB, and Gantz I (1999) Characterization of agouti-related protein binding to melanocortin receptors. Mol Endocrinol 13:148-155.