MCB Seminar - Prof.Dr. Stefan Knapp

The Medicinal Chemistry & Bioanalysis (MCB) Program GUIDE – Graduate School for Drug Exploration

SEMINAR

Prof.Dr. Stefan Knapp

Johann Wolfgang Goethe‐University, Institute for Pharmaceutical Chemistry, Frankfurt am Main, Germany

Chemical Probes as tools for target validation in cancer

For more information: a.s.s.domling@rug.nl (Alex Dömling)

Johann Wolfgang Goethe-University, Institute for Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Johann Wolfgang Goethe-University, Structural Genomics Consortium, Buchmann Institute for Life Sciences; Max-von-Laue-Str. 15, D-60438 Frankfurt am Main, Germany.

In my laboratory we are interested developing highly selective inhibitors, so called chemical probes for the validation of novel pharmacological targets. Since these reagents are used in mechanistic studies they need to be highly selective and comprehensively validated. To enable the development of probes we established a structural biology platform enabling family wide rational design. This effort led to an excellent structural coverage of the protein kinase family as well as of other target families such as bromodomains, small interaction domains that recognize acetylated lysine sequences in chromatin. In this talk I will summarize strategies that led to the development of new design strategies for highly selective inhibitors of protein kinases and will provide examples of novel targets validated by selective chemical tools.