Ligand Binding in the Transmembrane Region: of Metabotropic Glutamate Receptors-  Practical and Theoretical Investigations

Ligand Binding in the Transmembrane Region: of Metabotropic Glutamate Receptors- Practical and Theoretical Investigations

von Tobias Noeske
Taschenbuch - 9783639414929
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Beschreibung

Revision with unchanged content. Group I metabotropic glutamate receptors (mGluRs) play an important role in the treatment of numerous neurodegenerative, cognitive and psychiatric dis­orders. How can we identify exogenous ligands mediating the effects of mGluRs? How do these ligands affect the receptor? The author Tobias Noeske presents the establishment of strategies for the identification and optimization of molecules acting as non-competitive anta­gonists of group I mGluRs. These strategies ensure high diversity in the identi­fied chemotypes not resembling original reference molecules ("scaffold-hop­ping"). The detection of new scaffolds, in turn, is divided into two ap­proa­ches: First the development of pharmacological assays to screen com­pounds at a certain target for their bioactivity, and second the evaluation of com­pu­ter aided methods for the identification of virtual hits to be screened on the pharmacological assays. Promising molecules were optimized regarding bio­activity and selectivity, their binding mode investigated and, fi­nally, com­pared to existing lead compounds. This book addresses scientists in academia and industry working in early stage drug discovery, predominantly in computer aided drug design.

Details

Verlag AV Akademikerverlag
Ersterscheinung Mai 2012
Maße 220 mm x 150 mm x 12 mm
Gewicht 320 Gramm
Format Taschenbuch
ISBN-13 9783639414929
Auflage Nicht bekannt
Seiten 204

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