Selected Publications
- Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. T. Wagner, H. Greschik, T. Burgahn, K. Schmidtkunz, A.‑K. Schott, J. McMillan, L. Baranauskienė, Y. Xiong, O. Fedorov, J. Jin, U. Oppermann, D. Matulis, R. Schüle, M. Jung; Nucl. Acids Res. (2016) doi:10.1093/nar/gkw089.
- Assembly of methylated LSD1 and CHD1 drives AR dependent transcription and translocation. E. Metzger, D. Willmann, J. McMillan, I. Forne, P. Metzger, S. Gerhardt, K. Petroll, A. von Maessenhausen, S. Urban, A.-K. Schott, A. Espejo, A. Eberlin, D. Wohlwend, K. M. Schüle,
M. Schleicher, S. Perner, M. T. Bedford, M. Jung, J. Dengjel, R. Flaig, A. Imhof, O. Einsle,
R. Schüle; Nat. Struct. Mol. Biol. 23 (2016) 132-139. - Structure-based Development of a Sirtuin 2 Affinity Probe. M. Schiedel, T. Rumpf, B. Karaman, A. Lehotzky, S. Gerhardt, J. Ovádi, W. Sippl, O. Einsle, M. Jung; Angew. Chem. Int. Ed. 55 (2016) 2252-2256.
- Selective Sirt2-inhibition by ligand-induced rearrangement of the active site. T. Rumpf,
M. Schiedel, B. Karaman, C. Roessler, B. J. North, A. Lehotzky, J. Olah, K. I. Ladwein,
K. Schmidtkunz, M. Gajer, M. Pannek, C. Steegborn, D. A. Sinclair, S. Gerhardt, J. Ovadi,
M. Schutkowski, W. Sippl, O. Einsle, M. Jung, Nat. Commun. 6 (2015) 6263. - Synthesis and biological investigation of oxazole hydroxamates as highly selective histone deacetylase 6 (HDAC6) inhibitors. J. Senger, J. Melesina, M. Marek, C. Romier, I. Oehme,
O. Witt, W. Sippl, M. Jung; J. Med. Chem. 59 (2016) 1545–1555.
FRIAS Project
Chemical Epigenetics
Epigenetics is one of the major topics of modern biomedical research and is already a major focus in the Freiburg research landscape with international visibility. We will establish a Research Focus on Chemical Epigenetics that deals with epigenetic mechanisms on a molecular level using our combined expertise in synthetic organic and medicinal chemistry, structural biochemistry and bioinformatics to address this topic in a highly synergistic manner. The main scientific focus of our project will be acetyl and methyl lysine binding proteins, so called histone code readers. Structural analyses provide the basis for identification and optimization of new chemical ligands for these proteins in a rational, bioguided fashion. This will lead to new chemical tools that will allow dissecting cellular pathways involving these proteins as well as the analysis of their suitability as targets in drug discovery. The structural aim of this project is the preparation of a proposal for a structured PhD programme in Chemical Epigenetics with a strong international education perspective.