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Ligand Binding in the Transmembrane Region of Metabotropic Glutamate Receptors (Paperback)
Loot Price: R1,573
Discovery Miles 15 730
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Ligand Binding in the Transmembrane Region of Metabotropic Glutamate Receptors (Paperback)
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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.
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