BBB seminar: Manfred Jung
Chemical epigenetics - targeting reversible histone acetylation
Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Germany
Our research focus is `Chemical Epigenetics´ and deals with the development and application of chemical and biochemical tools to dissect biological pathways, to validate therapeutic targets and to discover and optimize potential drugs addressing a wide range of epigenetic targets. In this talk histone deacetylation by zinc dependent (HDACs) and NAD+-dependent enzymes (Sirtuins, esp. subtype Sirt2) is covered. We have developed a wide range of biochemical and biophysical assays for these targets which have identified new hits. These were subsequently optimized in a structure-guided fashion for potency and selectivity and were converted into functionalized tools for chemical biology. E.g., we have developed a biotinylated Sirt2 inhibitor for chemoproteomic studies and a proteolysis targeted chimera (PROTAC) based on thalidomide.
Chairperson: Jan Haavik, Department of Biomedicine