Article (Scientific journals)
Homology modeling of the serotoninergic 5-HT2c receptor
Farce, Amaury; Dilly, Sébastien; Yous, Said et al.
2006In Journal of Enzyme Inhibition and Medicinal Chemistry, 21, p. 285-292
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Keywords :
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 :
Laboratoire de Chimie Thérapeutique, Université de Lille 2
Disciplines :
Pharmacy, pharmacology & toxicology
Computer science
Author, co-author :
Farce, Amaury;  Université de Lille 2 > Faculté des Sciences Pharmaceutiques et Biologiques > Laboratoire de Chimie Thérapeutique
Dilly, Sébastien ;  Université de Lille 2 > Faculté des Sciences Pharmaceutiques et Biologiques > Laboratoire de Chimie Thérapeutique
Yous, Said;  Université de Lille 2 > Faculté des Sciences Pharmaceutiques et Biologiques > Laboratoire de Chimie Thérapeutique
Berthelot, Pascal;  Université de Lille 2 > Faculté des Sciences Pharmaceutiques et Biologiques > Laboratoire de Chimie Thérapeutique
Chavatte, Philippe;  Université de Lille 2 > philippe.chavatte@univlille2. fr > Laboratoire de Chimie Thérapeutique
Language :
English
Title :
Homology modeling of the serotoninergic 5-HT2c receptor
Publication date :
June 2006
Journal title :
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN :
1475-6366
eISSN :
1475-6374
Publisher :
TAYLOR & FRANCIS LTD, United Kingdom
Volume :
21
Pages :
285-292
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 09 June 2011

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