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 Forschungsbericht für das Jahr 2018

Institut für Pharmazeutische Wissenschaften

Arbeitskreis Prof. Dr. Manfred Jung

Albertstr. 23 (postalisch: Albertstr. 25)
79104 Freiburg
Tel: 203-4896
Email manfred.jung@pharmazie.uni-freiburg.de
http://www.jungm.de


Wissenschaftliche Mitarbeiterinnen und Mitarbeiter

  • Dr. Alexander Hauser, Leitender wissenschaftlicher Mitarbeiter (m/w), Akad. Rat
  • Dr. Nicolas Barthes, Postdoc (m/w)
  • Johannes Bacher, Doktorand (m/w)
  • Mirjam Hau, Doktorand (m/w)
  • Daniel Herp, Doktorand (m/w)
  • Eva-Maria Herrlinger
  • Daria Monaldi, Doktorand (m/w)
  • Johannes Seitz, Doktorand (m/w)
  • Roman Simon, Doktorand (m/w)
  • Sören Swyter, Doktorand (m/w)
  • Sandra Wenzler, Doktorand (m/w)
  • Natalie Wössner
Einträge in der Rubrik "Who is Who"

Forschungsschwerpunkte

  • Wirkstoffsynthese und Assay-Entwicklung im Bereich Epigenetik. Schwerpunkt: Histon-Deacetylasen, Histonacetyl- und methyltransferasen als neue Targets für die Krebstherapie

Finanzierung

  • Deutsche Krebshilfe
  • DFG: Ju 295/7-1
  • Wilhelm-Sander-Stiftung

Wissenschaftliche Publikationen

Originalarbeiten in wissenschaftlichen Fachzeitschriften:
  • Bayer T, Chakrabarti A, Lancelot J, Shaik TB, Hausmann K, Melesina J, Schmidtkunz K, Marek M, Erdmann F, Schmidt M, Robaa D, Romier D, Pierce RJ, Jung M, Sippl W: Synthesis, crystallization studies and in vitro characterization of novel cinnamic acid derivatives as SmHDAC8 inhibitors for the treatment of Schistosomiasis Chemmedchem, 2018. (in Druck)
  • Conrad, Simoben V, Robaa D, Chakrabarti A, Schmidtkunz K, Marek M, Lancelot J, Kannan S, Melesina J, Shaik TJ, Pierce R, Romier C, Jung M, Sippl W: A novel class of Schistosoma mansoni histone deacetylase 8 (HDAC8) inhibitors identified by structure-based virtual screening and in vitro testing Molecules, 2018; 23.
  • Daskalakis M, Brocks D, Sheng Y-H, Saiful Islam MD, Ressnerova A, Assenov Y, Milde T, Oehme I, Witt O, Goyal A, Kuehn A, Hartmann M, Weichenhan D, Jung M, Plass C: Reactivation of endogenous retroviral elements via treatment with DNMT- and HDAC-inhibitors Cell Cycle, 2018. (in Druck)
  • Heimburg T, Kolbinger FR, Zeyen P, Ghazy E, Herp D, Schmidtkunz K, Melesina J, Robaa D, Erdmann F, Schmidt M, Romier C, Witt O, Oehme I, Jung M, Sippl W: Structure-based design and biological characterization of selective HDAC8 inhibitors with anti-neuroblastoma activity J Med Chem, 2018. (in Druck)
  • Karaman B, Alhalabi Z, Swyter S, Mihigo SO, Andrae-Marobela K, Jung M, Sippl W, Ntie-Kang F: Identification of Bichalcones as Sirtuin Inhibitors by Virtual Screening and in Vitro Testing Molecules, 2018 (23). (in Druck)
  • King K, Hauser A-T, Melesina J, Sippl W, Jung M: Carbamates as prodrugs and new warhead for HDAC inhibition Molecules, 2018; 23: 321.
  • Kolbinger FR, Koeneke E, Ridinger J, Heimburg T, Müller M, Bayer T, Sippl W, Jung M, Gunkel N, Miller AK, Westermann F, Witt O, Oehme I: The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines Arch Toxicol, 2018. (in Druck)
  • Kolbinger FR, Wrobel J, Meder B, Distel M, Heimburg T, Sippl W, Jung M, Peterziel H, Kranz D, Boutros M, Westermann F, Witt O, Oehme I: A kinome-wide RNAi screen identifies ALK as a target to sensitize neuroblastoma cells for HDAC8-inhibitor treatment Cell Death Differ, 2018. (in Druck)
  • Lecointre B, Narozny R, Borello MT, Senger J, Chakrabarti A, Jung M, Marek M, Romier C, Melesina J, Sippl W, Bischoff L, Ganesan A: Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity Philos T R Soc B, 2018. (in Druck)
  • Robaa D, Monaldi D, Wössner N, Kudo N, Rumpf T, Schiedel M, Yoshida M, Jung M: Opening the selectivity pocket in the human lysine deacetylase Sirtuin2 – new opportunities, new questions Chem Rec, 2018. (in Druck)
  • Schiedel M, Herp D, Hammelmann s, Swyter s, Lehotzky A, Robaa D, Oláh J, Ovádi J, Sippl W, Jung M: Chemically induced degradation of sirtuin 2 (Sirt2) by a proteolysis targeting chimera (PROTAC) based on sirtuin rearranging ligands (SirReals) J Med Chem, 2018; 61: 482-481.
  • Schulz-Fincke J, Hau M, Barth J, Robaa D, Willmann D, Kürner A, Haas J, Greve G, Haydn T, Fulda S, Lübbert M, Lüdeke s, Berg T, Sippl W, Schüle R, Jung M: 148. Structure-activity studies on N-substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation Eur J Med Chem, 2018; 144: 52-67.
  • Simeth NA, Altmann L-M, Wössner N, Bauer E, Jung M, König B: Photochromic Indolyl Fulgimides as Chromo-Pharmacophores Targeting Sirtuins J Org Chem, 2018. (in Druck)
  • Waldschmidt J, Keller A, Ihorst G, Grishina O, Müller S, Wider D, Frey AV, King K, Simon RP, May AM, Tassone P, Duyster J, Jung M, Wäsch R, Engelhardt M: Safety and efficacy of vorinostat, bortezomib, doxorubicin and dexamethasone in a phase I/II study for relapsed or refractory multiple myeloma (VERUMM study: vorinostat in elderly, relapsed and unfit multiple myeloma) Haematologica, 2018. (in Druck)
Reviews/Übersichtsartikel in wissenschaftlichen Fachzeitschriften:
  • Schiedel M, Robaa D, Rumpf T, Sippl W, Jung M: The current state of NAD+-dependent histone deacetylases (sirtuins) as novel therapeutic targets (Review) Med Res Rev, 2018; 38 (online): 147-200. : http://10.1002/med.21436

Besondere wissenschaftliche Aktivitäten

Abschlussarbeiten