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Our research group is working on the medicinal-chemical development of subtype selective inhibitors of the four GABA transport proteins mGAT1 - mGAT4. As ligand-receptor interaction generally represents highly specific processes of recognition, our particular emphasis is on the synthesis and biological evaluation of enantiomerically pure compounds. We also develop new methods of synthesis, particularly asymmetric syntheses for the expression of test compound in enantiomerically pure form. The biological screening is conducted with radioligand binding assays and a new method employing mass spectrometry we have developed to assess the ligand-receptor interaction (MS-Binding Studies).The results of the biological assays are employed in molecular modeling to create structure-activity-relationships (SAR) and 3-D bond models, which then serve as a basis for further optimizations.

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