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Kurz group.
Heinrich-Heine-Universität Düsseldorf. Universitätsstr. 1, 40225 Düsseldorf, Germany

Histone deacetylases, HDAC inhibitors, prodrugs, synthesis, drug design


Our key expertise is the design and synthesis of selective histone deacetylase inhibitors


Synthetic tools: Conventional, microwave assisted and solid-phase synthesis

Collaborations outside COST

1. Dr. Benjamin Mordmüller, Univesity of Tübingen, Tübingen, Germany: Antiplasmodial activity of HDAC inhibitors 2. Assoc. Prof. Dr. Katherine Andrews, Griffith University, Brisbane, Australia: Antiplasmodial activity of HDAC inhibitors 3. Prof. Dr. Vicky M. Avery, Griffith University, Brisbane, Australia: Gametocytocidal activity of HDAC inhibitors 4. Prof. Dr. Elizabeth A. Winzeler, University of California, La Jolla, USA: Activity of HDAC inhibitors against Plasmodium liver stages 5. Prof. Dr. Holger Gohlke, Heinrich-Heine-Universität Düsseldorf, Germany: Structure-based design of HDAC inhibitors 6. Prof. Dr. Matthias U. Kassack, Heinrich-Heine-Universität Düsseldorf, Germany: Anticancer activity of HDAC inhibitors 7. Prof. Markus Fischer, University of Hamburg, Germany: Inhibition of the non-mevalonate isoprenoid biosynthesis. 8. Prof. InKyeom Kim, Kyungpook National University, Daegu, Korea: HDAC inhibition and metabolic syndrom, hypertension

Short description of ongoing research projects

1. Design and synthesis of isoform- and class-selective HDAC inhibitors 2. Development of parasite-selective antimalarial HDAC inhibitors with multistage activity 3. Inhibition of the non-mevalonate isoprenoid biosynthesis 4. Development of α-helix mimetics to inhibit protein-protein interactions 5. Development of prodrugs

  1. 1. Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. Histone Deacetylase Inhibitors with a Novel Connecting Unit Linker Region Reveal a Selectivity Profile for HDAC4 and HDAC5 with Improved Activity against Chemoresistant Cancer Cells. J. Med. Chem. 2013, 56, 427–436.
  2. 2. Kunfermann A, Lienau C, Illarionov B, Held J, Gräwert T, Behrendt CT, Werner P, Hähn S, Eisenreich W, Riederer U, Mordmüller B, Bacher A, Fischer M, Groll M, Kurz T. IspC as Target for Antiinfective Drug Discovery: Synthesis, Enantiomeric Separation, and Structural Biology of Fosmidomycin Thia Isosters. J. Med. Chem. 2013, 56, 8151-8162.
  3. 3. Trenholme K, Marek L, Duffy S, Pradel G, Fisher G., Hansen FK, Skinner-Adams TS., Butterworth A., Che Ngwa J, Moecking J, Goodman CD, McFadden GI, Sumanadasa SDM, Fairlie DP, Avery VM, Kurz T. and Andrews KT. Lysine acetylation in sexual stage malaria parasites is an epigenetic target for antimalarial small molecules. Antimicrob. Agents Chemother. 2014, 58, 3666-3678.
  4. 4. Spanier L, Ciglia E, Hansen FK, Kuna K, Frank W, Gohlke H, Kurz T. Design, synthesis and conformational analysis of trispyrimidonamides as α-helix mimetics. J. Org. Chem. 2014 79, 1582–1593.
  5. 5. Brücher, K, Gräwert, T, Konzuch, S, Held, J., Lienau, C, Berendt, C, Illarionov, B, Maes, L, Bacher, A, Wittlin, S, Mordmüller, B, Fischer, M, Kurz, T. Prodrugs of reverse Fosmidomycin Analogues. J. Med. Chem. 2015, 58, 2025-2035.
Other activities of potential interest to others

Cost UE