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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

In Silico Approaches Towards the Understanding of the Structure- Function Relationships in Metabotropic Glutamate Receptors (mGluRs) and other Family C GPRCs

Author(s): Gabriele Costantino

Volume 12, Issue 17, 2006

Page: [2159 - 2173] Pages: 15

DOI: 10.2174/138161206777585210

Price: $65

Abstract

Family C of the superfamily of G-protein coupled receptors is a growing family of heptahelical receptors, which includes, among others, metabotropic glutamate receptors (mGluRs) and GABA(B) receptors. A common feature of all the members of family C is a structural architecture much more complex than any other GPCRs. Computational studies, including homology modeling, pharmacophore definitions and molecular dynamics simulations have constantly flanked experimental approaches in the understanding of the receptor functioning. The present review will discuss the evolution of our perception in family C GPCRs structure and function as emerged from the critical comparison of in silico methods with molecular biology and crystallographic experiments.

Keywords: GPCRs, Metabotropic glutamate receptors, Venus flytrap, homology modeling, Extracellular domain


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