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Homology Modeling of 5-HT2C Receptors

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5-HT2C Receptors in the Pathophysiology of CNS Disease

Part of the book series: The Receptors ((REC,volume 22))

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Abstract

Achieving 5-HT2C selectivity is still a challenge for medicinal chemists. Luckily, they do not have to synthesize more or less blindly huge numbers of compounds hoping to obtain pharmacologically meaningful results since computational tools have been efficiently used to cope with this problem. 5-HT2C belongs to one of the largest drug target class, the G-protein-coupled receptors (GPCR). This makes it amenable to homology modeling, a computational method for building a three-dimensional structural model in order to study at an atomic level the interactions with its ligands. It would have been impossible to propose any meaningful model without an initial dataset, the crystallographic structure of bovine rhodopsin. However, this template was only the primer for more involved in silico refinements of the putative basal state of 5-HT2C to extract from a list of spatial position of atoms the possible binding modes of neutral antagonists, agonists, and even inverse agonists. The history of 5-HT2C modeling and its application to the generation of hypothesis on the selectivity toward 5-HT2C will be discussed, from the alignment between the templates and human 5-HT2C sequences through the hypothesis of binding sites to the more recent insights gained into selectivity by relating spatial position of the critical residues with their conservation through homologous sequences. A GPCR modeling review would not be complete without some discussion of the complex dynamics of their activation and the peculiar difficulties it poses for computational chemists.

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  1. Laboratoire de Chimie Thérapeutique, Université de Lille 2, EA 1043, 3 Rue du Professeur Laguesse, B.P. 83, F-59006, Lille, France

    Philippe Chavatte

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  1. Nicolas Renault
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  2. Amaury Farce
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  3. Philippe Chavatte
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Correspondence to Philippe Chavatte .

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  1. , Department of Physiology and Biochemistr, University of Malta, Msida, Malta, MSD 2080, Italy

    Giuseppe Di Giovanni

  2. Centro di Ricerche Farmacologiche e, Biomediche, Consorzio Mario Negri Sud, Via Nazionale 8, Santa Maria Imbaro, 66030, Chieti, Italy

    Ennio Esposito

  3. Centro di Ricerche Farmacologiche e, Biomediche, Consorzio Mario Negri Sud, Via Nazionale 8, Santa Maria Imbaro, 66030, Chieti, Italy

    Vincenzo Di Matteo

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Renault, N., Farce, A., Chavatte, P. (2011). Homology Modeling of 5-HT2C Receptors. In: Di Giovanni, G., Esposito, E., Di Matteo, V. (eds) 5-HT2C Receptors in the Pathophysiology of CNS Disease. The Receptors, vol 22. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60761-941-3_6

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