Tobias Noeske Livres

Focusing on the identification and optimization of non-competitive antagonists for group I metabotropic glutamate receptors (mGluRs), this work by Tobias Noeske explores innovative strategies that promote a diverse range of chemotypes. It details the development of pharmacological assays to assess compound bioactivity and the use of computer-aided methods to identify potential candidates. The research emphasizes optimizing promising molecules for bioactivity and selectivity, making it a valuable resource for scientists in early-stage drug discovery and computer-aided drug design.

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 detection and optimization of molecules acting as non-competitive antagonists of group I mGluRs. These strategies guarantee 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.