Martin Luther University Halle-Wittenberg

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Publications 2016

R. P. Simon, D. Robaa, Z. Al Halabi, W. Sippl and M. Jung. KATching-up on Histone Acetyltransferase Inhibitors. J. Med. Chem. 59, 1249–1270, 2016. DOI:10.1021/acs.jmedchem.5b01502   

L.  Motlagh, R. Golbik, W. Sippl, S. Zierz. Malony-CoA inhibits the S113L variant of carnitine-D. Robaa, T. Wagner, C. Luise, L. Carlino, J. McMillan, R. Flaig, R. Schüle, M. Jung, and W. Sippl. Identification and SAR studies of Small-Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1. ChemMedChem. 11, 2327-2338, 2016. doi:10.1002/cmdc.201600362.   

D. Ostrovskyi D, Rumpf T, Eib J, Lumbroso A, Slynko I, Klaeger S, Heinzlmeir S, Forster M, Gehringer M, Pfaffenrot E, Bauer SM, Schmidtkunz K, Wenzler S, Metzger E, Kuster B, Laufer S, Schüle R, Sippl W, Breit B, Jung M. Tofacitinib and analogues as inhibitors of the histone kinase PRK1 (PKN1). Future Med Chem. 8(13):1537-51, 2016. DOI:10.4155/fmc-2016-0132   

A. Chakrabarti, J. Melesina, F. Kolbinger, I. Oehme, J. Senger, O. Witt, W. Sippl, M. Jung. Targeting histone deacetylase 8 (HDAC8) as a therapeutic approach to cancer and neurodegenerative diseases. Future Med Chem. 8(13):1609-34, 2016. DOI:10.4155/fmc-2016-0117   

C. Hempel, A. Najjar, F. Totzke, C. Schächtele, W. Sippl, C. Ritter, and A. Hilgeroth. Discovery of dually acting small-molecule inhibitors of cancer-resistance relevant receptor tyrosine kinases EGFR and IGF-1R. Med. Chem. Commun. 7, 2159-2166, 2016. DOI:10.1039/C6MD00329J   

I. Slynko, T. Rumpf, S. Klaeger, Heinzlmeier, A. Najar, B. Küster, R. Schüle, M. Jung, W. Sippl. Identification of highly potent PRK1 inhibitors by virtual screening, binding free energy rescoring and in vitro testing. ChemMedChem. 11(18):2084-94, 2016. doi:10.1002/cmdc.201600284   

F. Ntie-Kang, C. V. Simoben, B. Karaman, V. F. Ngwa, L. L. Lifongo, P. N. Judson , W. Sippl and L. M. Mbaze. Pharmacophore Modeling and in Silico Toxicity Assessment of Potential Anticancer Agents from African Medicinal Plants. Drug Des Devel Ther. 10:2137-54, 2016. doi:10.2147/DDDT.S108118.    eCollection 2016.

V. Tell, M. Holzer, I. Slynko, W. Sippl, A. Hilgeroth. Multitargeting drug development in alzheimers disease: approaches with  novel benzo[4,5]furo[2,4-b]pyridines as protein kinase inhibitors. Curr Alzheimer Res. 13(12):1330-1336, 2016.

T. Heimburg, A. Chakrabarti, M. Marek, J. Lancelot, J. Melesina, D. Robaa, F. Erdmann, M. Schmidt, R. J. Pierce, C. Romier, M. Jung and W. Sippl. Structure-Based Design and Synthesis of Novel Inhibitors targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis. J. Med. Chem. 59, 2423–2435, 2016. DOI:10.1021/acs.jmedchem.5b01478   

Q. Y. Zhu, Zhou, C. Chen, S. Heinemann, R. El-Mergawy, R. Schönherr, D. Robaa, W. Sippl, G. Scriba. Stereospecific capillary electrophoresis assays using pentapeptide substrates for the study of Aspergillus nidulans methionine sulfoxide. Electrophoresis 37(14):2083-90, 2016. doi:10.1002/elps.201600181   

F. Ntie-Kang, L.  E. Njume, Y. I. Malange, S.  Günther, W. Sippl, J. N. Yong. The chemistry and biological activities of natural products from Northern African plant families: From Taccaceae to Zygophyllaceae. Nat. Prod. Bioprospect. 6(2):63-96, 2016. DOI:10.1007/s13659-016-0091-9   

M. Roatsch, D. Robaa, M. Pippel, J. E. Nettleship, Y. Reddivari, L. E. Bird, I. Hoffmann, H. Franz, R. J. Owens, R. Schüle, R. Flaig, W. Sippl, M. Jung. Substituted 2-(2-aminopyrimidin-4-yl)pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone demethylases. Future Med Chem. 8(13):1553-71, 2016. DOI:10.4155/fmc.15.188   

L. Motlagh, R. Golbik, W. Sippl, S. Zierz. Stabilization of the thermolabile variant S113L of carnitine palmitoyltransferase II. Neurology: Genetics, ;2(2):e53, 2016. doi:10.1212/NXG.0000000000000053.   

B. Karaman, M. Jung, W. Sippl Structure-based design and computational studies of sirtuin inhibitors. in: Epi-Informatics: Discovery and Development of Small Molecule Epigenetic Drugs and Probes (Ed.: J. L. Medina-Franco) 2016

T. Wagner, D. Robaa, W. Sippl, M. Jung Epigenetic Readers Interpreting the Lysine Methylome - Biological Roles and Drug Discovery, in: Drug Discovery in Cancer Epigenetics (Eds.: G. Egger, P. Arimondo) 273-304, 2016

J. Senger, J. Melesina, M. Marek, C. Romier, I. Oehme, O. Witt, W. Sippl and M. Jung. Synthesis and biological investigation of new selective histone deacetylase 6 (HDAC6) inhibitors. J. Med. Chem. 59, 1545-55, 2016. DOI:10.1021/acs.jmedchem.5b01493   

M. Schiedel, T. Rumpf, B. Karaman, A. Lehotzky, S. Gerhardt, J. Ovádi, W. Sippl, O. Einsle, M. Jung. Structure-based Development of a Sirtuin 2 Affinity Probe. Angew. Chem. Int. Ed. Engl.  55, 2252-6, 2016. doi:10.1002/anie.201509843   

G. Tangherlinia, T. Torregrossa, O. Agoglitta, J. Melesina, W. Sippl, R. Holl. Synthesis and biological evaluation of enantiomerically pure glyceric acid derivatives as LpxC inhibitors. Bioorg. Med. Chem. Lett. 24,1032-44, 2016. doi:10.1016/j.bmc.2016.01.029   .

M. Schiedel, T. Rumpf, B. Karaman, A. Lehotzky, S. Gerhardt, J. Ovádi, W. Sippl, O. Einsle, M. Jung. Aminothiazoles as potent and selective Sirt2 inhibitors – a structure-activity relationship study. J. Med. Chem. 59, 1599–1612, 2016. DOI:10.1021/acs.jmedchem.5b01517   

L.  Motlagh, R. Golbik, W. Sippl, S. Zierz. Malony-CoA inhibits the S113L variant of carnitine-palmitoyltransferase II. Biochim Biophys Acta. 1861, 34-40, 2016. doi:10.1016/j.bbalip.2015.10.005