5-HT2c receptor; GPCRs, homology modelling; agomelatine; depression; MASSA
Abstract :
[en] Since its discovery, 5-hydroxytryptamine, more usually called serotonin, has been an elusive candidate as a major mood regulator. This capacity gives it a great importance in the treatment of depression. It is within this framework that our work takes place, as it is related more particularly to a new therapeutic class whose leader is agomelatine. This compound binds to the melatoninergic receptors and to the serotoninergic 5-HT2c receptor, giving rise to the MASSA concept (Melatonin Agonist and Selective Serotonin Antagonist). Like the majority of the serotoninergic receptors, the sub-type 5-HT2c is a G-protein coupled receptor (GPCR). The three-dimensional structure of 5-HT2c is not experimentally known, and we thus resorted to comparative homology modelling to build a model allowing us to study its interactions with agomelatine.
Research Center/Unit :
Laboratoire de Chimie Thérapeutique, Université de Lille
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Bibliography
Dalgliesh, CE and Toh, CC and Work, TS. (1953) J Physiol, 120, pp. 298-310.
Yamamoto, K and Nohara, K and Furuya, T and Yamatodani, A. (2005) Pharmacol Biochem Behav, 82, pp. 24-29.
Cazzola, I and Matera, MG. (2000) Trends Pharmacol Sci, 21, pp. 13-16.
Garabette, ML and Martin, KF and Redfern, PH. (2000) Br J Pharmacol, 131, pp. 1569-1576.
Coppen, AJ and Doogan, DP. (1998) J Clin Psychiatry, 49, pp. 4-11.
Moskowitz, DS and Pinard, G and Zuroff, DC and Annable, L and Young, SN. (2003) Adv Exp Med Biol, 527, pp. 215-224.
Holden, JE and Naleway, FE and Jeong, Y. (2005) Neuroscience, 135, pp. 1255-1268.
Reis, LC and Almeida, AC and Cedraz-Mercez, PL and Olivares, EL and Marinho, A, Jr and Thomaz, CM. (2005) Braz J Biol, 65, pp. 353-361.
Saadat, KS and O'shea, E and Colado, MI and Elliott, JM and Green, AR. (2005) Psychopharmacology (Berl), 179, pp. 884-890.
Hoyer, D and Hannon, JP and Martin, GR. (2002) Pharmacol Biochem Behav, 71, pp. 533-554.
Ballesteros, JA and Jensen, AD and Liapakis, G and Rasmussen, SG and Shi, L and Gether, U and Javitch, JA. (2001) J Biol Chem, 276, pp. 29171-29177.
White, SH and Ladokhin, AS and Jayasinghe, S and Hristova, K. (2001) J Biol Chem, 276, pp. 32395-32398.
Stenkamp, RE and Teller, DC and Palczewski, K. (2005) Arch Pharm Chem Life Sci, 338, pp. 209-216.
Archer, E and Maigret, B and Escrieut, C and Pradayrol, L and Fourmy, D. (2003) Trends Pharmacol Sci, 24, pp. 36-40.
Millan, MJ and Gobert, A and Lejeune, F and Dekeyne, A and Newman-Tancredi, A and Pasteau, V and Rivet, JM and Cussac, D. (2003) J Pharmacol Exp Ther, 306, pp. 954-964.
Chilman-Blair, K and Castañer, J and Bayès, M and Silvestre, JS. (2003) Drugs Future, 28, pp. 7-13.
Depreux, P and Lesieur, D and DAit Mansour, H and Morgan, P and Howell, HE and Renard, P and Caignard, DH and Pfeiffer, B and Delagrange, P and Guardiola, B and Yous, S and Demarque, A and Adam, G and Andrieux, J. (1994) J J Med Chem, 37, pp. 3231-3239.
SYBYL 6.9.1, Tripos Inc, 1699 South Hanley Road, St. Louis, MO 63144-2913, U.S.A
Lesk, AM and Chothia, C. (1986) Philos Trans R Soc Lond B Biol Sci, 317, pp. 345-356.
Wu, CH and Yeh, LS and Huang, H and Arminski, L and Castro-Alvear, J and Chen, Y and Kourtesis, P and Ledley, RS and Suzek, BE and Vinayaka, CR and Zhang, J and Barker, WC. (2003) Nucleic Acids Res, 31, pp. 345-347.
Nathans, J and Hogness, DS. (1983) Cell, 34, pp. 807-814.
Saltzman, AG and Morse, B and Whitman, MM and Ivanshchenko, Y and Jaye, M and Felder, S. (1991) Biochem Biophys Res Commun, 181, pp. 1469-1478.
Thompson, JP and Gibson, TJ and Plewniak, F and Jeanmougin, F and Higgins, DG. (1997) Nucleic Acids Res, 24, pp. 4876-4882.
Berman, HM and Westbrook, J and Feng, Z and Gary, G and Bhat, TN and Weissig, H and Shindyalov, IN and Bourne, PE. (2000) Nucleic Acids Res, 28, pp. 235.
Okada, T and Sugihara, M and Bondar, AN and Elstner, M and Entel, P and Buss, V. (2004) J Mol Biol, 10, pp. 71-83.
Petrey, D and Xiang, Z and Tang, CL and Xie, L and Gimpelev, M and Mitros, T and Soto, CS and Goldsmith-Fischman, S and Kernytsky, A and Schlessinger, A and Koh, IYY and Alexov, E and Honig, B. (2003) Proteins: Struct Func and Genet, 53, pp. 430-435.
Pearlman, DA and Case, DA and Caldwell, JW and Ross, WR and Cheatham, DeBoltS, III TE and Ferguson, D and Seibel, G and Kollman, P. (1995) Comp Phys Commun, 91, pp. 1-41.
Ponder, JW and Case, DA. (2003) Adv Prot Chem, 66, pp. 27-85.
Laskowski, RA and Moss, DS and Thornton, JM. (1993) J Mol Biol, 231, pp. 1049-1067.
Clark, M and Cramer, V, III RD and an Opdenbosch, N. (1989) J Comp Chem, 10, pp. 982-1012.
Rashid, M and Manivet, P and Nishio, H and Pratuangdejkul, J and Rajab, M and Ishiguro, M and Launay, JM and Nagatomo, T. (2003) Life Sci, 73, pp. 193-207.
Jones, G and Willet, P and Glen, RC. (1995) J Mol Biol, 245, pp. 43-53.
Jones, G and Willet, P and Glen, RC and Leach, AR and Taylor, R. (1997) J Mol Biol, 267, pp. 727-748.
Wang, R and Lai, L and Wang, S. (2002) J Comp-Aided Mol Des, 16, pp. 11-26.
Okada, T. (2004) Biochem Soc Trans, 32, pp. 738-741.
Burris, KD and Breeding, M and Sanders-Bush, E. (1991) J Pharmacol Exp Ther, 258, pp. 891-896.
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