Martin-Luther-Universität Halle-Wittenberg

Publikationen 2018

Weitere Informationen zu den Publikationen der AG Prof. Sippl finden sie hier:

T. Bayer, A. Chakrabarti, J. Lancelot, T. B. Shaik, K. Hausmann, J. Melesina, K. Schmidtkunz, M. Marek, F. Erdmann, M. Schmidt, D. Robaa, C. Romier, R. J. Pierce, M. Jung and W. Sippl. Synthesis, crystallization studies and in vitro characterization of novel cinnamic acid derivatives as SmHDAC8 inhibitors for the treatment of Schistosomiasis. Chem Med Chem, 2018 May 27. doi:10.1002/cmdc.201800238   .

C. Schräder, A. Heinz, P. Majovsky, B. Karaman, J. Brinckmann, W. Sippl, and C. Schmelzer. Elastin is heterogeneously cross-linked. J. Bio. Chem., accepted.

C. Luise, D. Robaa. Application of Virtual Screening Approaches for the Identification of Small Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1. Methods Mol Biol. 2018;1824:347-370. doi:10.1007/978-1-4939-8630-9_21.   

A.T. Hauser, D. Robaa, M. Jung. Epigenetic small molecule modulators of histone and DNA methylation. Curr Opin Chem Biol. 2018 Aug;45:73-85. doi:10.1016/j.cbpa.2018.03.003.   

Robaa D, Monaldi D, Wössner N, Norio, Kudo, 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 Jun 21. doi:10.1002/tcr.201800044   .

J. Melesina, L. Praetorius, C. V. Simoben, D. Robaa, W. Sippl. Design of Selective HDAC Inhibitors: Rethinking Classical Pharmacophore. Future Med. Chem. 10, 1537-1540, 2018.

F. R. Kolbinger; E. Koeneke; J. Ridinger; T. Heimburg; T. Bayer; W. Sippl; M. Jung; N. Gunkel; A. K. Miller; O. Witt; I. Oehme. The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines. Arch. Toxicol. 92, 2649-2664, 2018. doi:10.1007/s00204-018-2234-8   

C. Platzer, A. Najjar; A. Rohe, F. Erdmann, W. Sippl, M. Schmidt. Identification of PKMYT1 Inhibitors by Screening the GSK Published Protein Kinase Inhibitor Set I and II. Bioorg. Med. Chem. 26, 4014-4024, 2018. doi:10.1016/j.bmc.2018.06.027   

B. Karaman, W. Sippl. Computational Drug Repurposing: Current Trends.
Curr Med Chem. 2018 May 29. doi:10.2174/0929867325666180530100332.   

C. V. Simoben, S. H. Akone, F. Ntie-KAng, W. Sippl. Compounds from African medicinal plants with activities against protozoal diseases: schistosomiasis, trypanosomiasis and leishmaniasis. Nat Prod Bioprospect. 2018 May 9. doi:10.1007/s13659-018-0165-y.   

A. Ripperger, A. Krischer, D. Robaa, W. Sippl, R. A. Benndorf. Pharmacogenetic Aspects of the Interaction of AT1 Receptor Antagonists With ATP-Binding Cassette Transporter ABCG2. Front. Pharmacol. 9, 463, 2018. DOI10.3389/fphar.2018.00463

S. Swyter, M. Schiedel, D. Monaldi, A. Lehotzky, T. Rumpf, J. Ovádi, W. Sippl, M. Jung. New chemical tools for probing activity and inhibition of the NAD+ dependent lysine deacylase sirtuin. Phil. Trans. R. Soc. B 373, 20170083, 2018. DOI:10.1098/rstb.2017.0083   

R. Narozny, B. Lecointre, J. Senger, A. Chakrabarti, M. Jung, M. Marek, C. Romier, J. Melesina, W. Sippl, M. T. Borrello, L. Bischoff, A. Ganesan.   Isoform selective HDAC6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity. Phil. Trans. R. Soc. B  373, 20170364, 2018. DOI:10.1098/rstb.2017.0364   

M. J. Chua, D. Robaa, T. S. Skinner-Adams, W. Sippl and K. T Andrews. Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites. International Journal for Parasitology: Drugs and Drug Resistance, 8, 189-193, 2018. doi:10.1016/j.ijpddr.2018.03.001   

C. V. Simoben, D. Robaa, A. Chakrabarti, K. Schmidtkunz, M. Marek, J. Lancelot, S. Kannan, J. Melesina, T. B. Shaik, R. J. Pierce, C. Romier, M. Jung and W. Sippl. A novel class of Schistosoma mansoni histone deacetylase 8 (HDAC8) inhibitors identified by structure-based virtual screening and in vitro testing. Molecules 23(3). pii: E566. doi:10.3390/molecules23030566    

D. Kalbas, S. Liebscher, T. Nowak, M. Meleshin, M. Pannek, C. Popp, Z. Alhalabi, F. Bordusa, W. Sippl, C. Steegborn, M. Schutkowski. Potent and selective inhibitors of human Sirtuin 5. J. Med. Chem., 61, 2460-2471, 2018  doi:10.1021/acs.jmedchem.7b01648   .

J. Shen, S. Najafi, S. Stäble, J. Fabian, E. Koeneke, F. R. Kolbinger, J. Wrobel, B. Meder, M. Distel, T. Heimburg, W. Sippl, M. Jung, H. Peterziel,, D. Kranz, M. Boutros, F. Westermann, O. Witt, I. Oehme. A kinome-wide RNAi screen identifies ALK as a target to sensitize neuroblastoma cells for HDAC8-inhibitor treatment. Cell Death Diff, DOI:10.1038/s41418-018-0080-0   

B. Karaman, Z. Alhalabi, S. Swyter, S. O. Mihigo, K. Andrae-Marobela, M. Jung, W. Sippl, F. Ntie-Kang. Identification of Bichalcones as Sirtuin Inhibitors by Virtual Screening and in Vitro Testing. Molecules, 23, 416, 2018. doi:10.3390/molecules23020416   

K. King,  A.-T. Hauser, J. Melesina, W. Sippl and M. Jung. Carbamates as prodrugs and new warhead for HDAC inhibition. Molecules, 23, 321, 2018. doi:10.3390/molecules23020321.   

L. Temme, B. Frehland, D. Schepmann, D. Robaa, W. Sippl, B. Wünsch. Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation. Eur. J. Med. Chem. 144, 672-681, 2018.  doi:10.1016/j.ejmech.2017.12.054   

J. Schulz-Fincke, M. Hau, J. Barth, D. Robaa, D. Willmann, A. Kürner, J. Haas, G. Greeve, T. Haydn, S. Fulda, E. Metzger, M. Lübbert, S. Lüdeke, T. Berg, W. Sippl, R. Schüle, and M. Jung. Structure-Activity Studies on N-Substituted Tranylcypromine Derivatives Lead to Selective 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. 144, 52-67, 2018.   

T. Fischer, A. Najjar, F. Totzke, C. Schächtele, W. Sippl , C. Ritter, A. Hilgeroth. Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance. J Enzyme Inhib Med Chem. 33, 1-8, 2018. doi:10.1080/14756366.2017.1370583   

A. C. Mora Huertas, C. E. H. Schmelzer, C. Luise, W. Sippl, M. Pietzsch, W. Hoehenwarter, A. Heinz. Degradation of tropoelastin and skin elastin by neprilysin. Biochimie 146, 73-78, 2018.

M. Schiedel, D. Herp, S. Hammelmann, S. Swyter, A. Lehotzky, D Robaa, J. Oláh, J. Ovádi, W. Sippl,  M. Jung. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J. Med. Chem. 61, 482-491, 2018. doi:10.1021/acs.jmedchem.6b01872   . Commented in Science "In the Pipeline   ".

M. Schiedel, D. Robaa, T. Rumpf, W. Sippl, M. Jung. The Current State of NAD+-Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets. Med. Res. Rev. 38(1), 147-200, 2018. doi:10.1002/med.21436.   

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