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Ligand Binding in the Transmembrane Region of Metabotropic Glutamate Receptors

Tobias Noeske

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ISBN 10: 3836423375 / ISBN 13: 9783836423373
Published by VDM Verlag Dr. Mueller e.K.
New Condition: New Soft cover
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204 pages. Dimensions: 9.6in. x 6.7in. x 0.4in.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. This item ships from multiple locations. Your book may arrive from Roseburg,OR, La Vergne,TN. Bookseller Inventory # 9783836423373

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Bibliographic Details

Title: Ligand Binding in the Transmembrane Region ...

Publisher: VDM Verlag Dr. Mueller e.K.

Binding: Paperback

Book Condition:New

Book Type: Paperback

About this title

Synopsis:

Group I metabotropic glutamate receptors (mGluRs) play an important role in the treatment of numerous neurodegenerative, cognitive and psychiatric dis觔rders. 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 anta茆onists of group I mGluRs. These strategies ensure high diversity in the identi苯ied chemotypes not resembling original reference molecules ("scaffold-hop計ing"). The detection of new scaffolds, in turn, is divided into two ap計roa苞hes: First the development of pharmacological assays to screen com計ounds at a certain target for their bioactivity, and second the evaluation of com計u負er aided methods for the identification of virtual hits to be screened on the pharmacological assays. Promising molecules were optimized regarding bio苔ctivity and selectivity, their binding mode investigated and, fi要ally, com計ared to existing lead compounds. This book addresses scientists in academia and industry working in early stage drug discovery, predominantly in computer aided drug design.

About the Author:

Research Scientist. Study of Pharmaceutics at the Goethe-Universit酹 in Frankfurt am Main, Germany. PhD-Thesis at Merz Pharmaceuticals GmbH, Frankfurt am Main, Germany. Post-doc at AstraZeneca, M闤ndal, Sweden.

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