Screening Unit

Publications

 

Anumala UR, Waaler J, Nkizinkiko Y, Ignatev A, Lazarow K, Lindemann P, Olsen PA, Murthy S, Obaji E, Majouga AG, Leonov S, von Kries JP, Lehtiö L, Krauss S, Nazaré M. (2017). Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach. J Med Chem. 60(24):10013-10025.

Fetzer C, Korotkov VS, Thänert R, Lee KM, Neuenschwander M, von Kries JP, Medina E, Sieber SA. (2017). A Chemical Disruptor of the ClpX Chaperone Complex Attenuates the Virulence of Multidrug-Resistant Staphylococcus aureus. Angew Chem Int Ed Engl. 56(49):15746-15750.

Igual Gil C, Jarius M, von Kries JP, Rohlfing AK. (2017). Neuronal Chemosensation and Osmotic Stress Response Converge in the Regulation of aqp-8 in C. elegans. Front Physiol. 8:380.

Juneja M, Kobelt D, Walther W, Voss C, Smith J, Specker E, Neuenschwander M, Gohlke BO, Dahlmann M, Radetzki S, Preissner R, von Kries JP, Schlag PM, Stein U. (2017). Statin and rottlerin small-molecule inhibitors restrict colon cancer progression and metastasis via MACC1. PLoS Biol. 15(6):e2000784.

Carter DM, Specker E, Przygodda J, Neuenschwander M, von Kries JP, Heinemann U, Nazaré M, Gohlke U. (2017). Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells. SLAS Discov. 22(7):801-812.

Hinderlich S, Neuenschwander M, Wratil PR, Oder A, Lisurek M, Nguyen LD, von Kries JP, Hackenberger CPR. (2017) Small Molecules Targeting Human N-Acetylmannosamine Kinase. Chembiochem. 18(13):1279-1285.

Wetzel C, Pifferi S, Picci C, Gök C, Hoffmann D, Bali KK, Lampe A, Lapatsina L, Fleischer R, Smith ES, Bégay V, Moroni M, Estebanez L, Kühnemund J, Walcher J, Specker E, Neuenschwander M, von Kries JP, Haucke V, Kuner R, Poulet JF, Schmoranzer J, Poole K, Lewin GR. (2017) Small-molecule inhibition of STOML3 oligomerization reverses pathological mechanical hypersensitivity. Nat Neurosci. 20(2):209-218.

Chenge JT, Duyet LV, Swami S, McLean KJ, Kavanagh ME, Coyne AG, Rigby SE, Cheesman MR, Girvan HM, Levy CW, Rupp B, von Kries JP, Abell C, Leys D, Munro AW. (2017). Structural Characterization and Ligand/Inhibitor Identification Provide Functional Insights into the Mycobacterium tuberculosis Cytochrome P450 CYP126A1. J Biol Chem. 292(4):1310-1329.

Du J, Neuenschwander M, Yu Y, Däbritz JH, Neuendorff NR, Schleich K, Bittner A, Milanovic M, Beuster G, Radetzki S, Specker E, Reimann M, Rosenbauer F, Mathas S, Lohneis P, Hummel M, Dörken B, von Kries JP, Lee S, Schmitt CA. (2017). Pharmacological restoration and therapeutic targeting of the B-cell phenotype in classical Hodgkin lymphoma. Blood. 129(1):71-81.

Wetzel C, Pifferi S, Picci C, Gök C, Hoffmann D, Bali KK, Lampe A, Lapatsina L, Fleischer R, Smith ES, Bégay V, Moroni M, Estebanez L, Kühnemund J, Walcher J, Specker E, Neuenschwander M, von Kries JP, Haucke V, Kuner R, Poulet JF, Schmoranzer J, Poole K, Lewin GR. (2016) Small-molecule inhibition of STOML3 oligomerization reverses pathological mechanical hypersensitivity. Nat Neurosci. 2016 Dec 12. doi: 10.1038/nn.4454. 

Fang L, Zhu Q, Neuenschwander M, Specker E, Wulf-Goldenberg A, Weis WI, von Kries JP, Birchmeier W. (2016). A small-molecule antagonist of the β-catenin/TCF4 interaction blocks the self-renewal of cancer stem cells and suppresses tumorigenesis. CANRES. 76:891-901.

Khatri Y, Ringle M, Lisurek M, von Kries JP, Zapp J, Bernhardt R. (2016) Substrate Hunting for the Myxobacterial CYP260A1 Revealed New 1α-Hydroxylated Products from C-19 Steroids. Chembiochem.  17(1):90-101.

Hu, H.-Y.; Lim, N.-H.; Juretschke, H.-P.; Ding-Pfennigdorf, D.; Florian, P.; Kohlmann, M., Kandira, A.; von Kries, J. P.; Saas, J.; Rudolphi, K. A.; Wendt, K. U.; Nagase, H.; Plettenburg, O.; Nazaré, M.; Schultz, C. (2015) In vivo visualization of osteoarthritic hypertrophic lesions. Chem. Sci., 6, 6256-6261.

Grosskopf, S., Eckert, C., Arkona, C., Radetzki, S., Böhm, K., Heinemann, U., Wolber, G., Kries, von, J.-P., Birchmeier, W., and Rademann, J. (2015). Selective inhibitors of the protein tyrosine phosphatase SHP2 block cellular motility and growth of cancer cells invitro and invivo. ChemMedChem 10, 815–826.

F. K. Voss, F. Ullrich, J. Münch, K. Lazarow, D. Lutter, N. Mah, MA. Andrade-Navarro, JP. von Kries, T. Stauber, and TJ. Jentsch. (2014) Identification of LRRC8 Heteromers as an Essential Component of the Volume-Regulated Anion Channel VRAC. Science 344: 634-8.

Bogum J, Faust D, Zühlke K, Eichhorst J, Moutty MC,Furkert J, Eldahshan A, Neuenschwander M, von Kries JP, Wiesner B, Trimpert C, Deen PMT, Valenti G, Rosenthal W, and Klussmann E. (2013) Small molecule screening to reveal mechanisms underlying aquaporin-2 trafficking. JASN 24:744-58.

Nagel D, Spranger S,Vincendeau M, Grau M, Raffegerst S, Kloo B, Hlahla D, Neuenschwander M, von Kries JP, Hadian K, Dörken B, Lenz P, Lenz G, Schendel DJ, and Krappmann D (2012). Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL. Cancer Cell 22: 825-37.

Habermann K, Mirgorodskaya E, Gobom J, Lehmann V, Müller H, Blümlein K, Deery MJ, Czogiel I, Erdmann C, Ralser M, von Kries JP, Lange BM. (2012) Functional analysis of centrosomal kinase substrates in Drosophila melanogaster reveals a new function of the nuclear envelope component otefin in cell cycle progression. Mol Cell Biol. 32:3554-69.

Kamper C, Korpis K, Specker E, Anger L, Neuenschwander M, Bednarski PJ, Link A. Sustainable synthesis and automated deposition: an accessible discovery screening library of fragment-like purines. Mol. Divers. 2012, 16, 541-551.

Waaler J, Machon O, Tumova L, Dinh H, Korinek V, Wilson SR, Paulsen JE, Pedersen NM, Eide TJ, Machonova O, Gradl D, Voronkov A, von Kries JP, Krauss S. A Novel Tankyrase Inhibitor Decreases Canonical Wnt Signaling in Colon Carcinoma Cells and Reduces Tumor Growth in Conditional APC Mutant Mice. Cancer Res. 2012, 72: 2822-32.

von Kleist, L., Stahlschmidt, W., Bulut, H., Gromova, K., Puchkov, D., Robertson, MJ., MacGregor, KA., Tomlin, N., Pechstein, A., Chau, N., Chircop, M., Sakoff, J., von Kries, JP., Saenger, W., Kräusslich, H-G., Shupliakov, O., Robinson,PJ., McCluskey, A., and Haucke V. Essential Role of the Clathrin Terminal Domain in Regulating Coated Pit Dynamics Revealed by Small Molecule Inhibition. Cell, 2011, 146 (3), 471-484.

Timm, T., von Kries, JP., Li, X., Mandelkow, E. und Mandelkow, E-V. Microtubule affinity regulating kinase (MARK) activity in living neurons examined by a genetically encoded FRET/FLIM based biosensor: Inhibitors with therapeutic potential. J. Biol. Chem., 2011, 286, 41711-41722. 

Linden, AH., Lange, S., Franks, TW., Akbey, Ü., Specker, E., van Rossum, B-J., Oschkinat, H., Neurotoxin II Bound to Acetylcholine Receptors in Native Membranes Studied by Dynamic Nuclear Polarization NMR. JACS, 2011, 133 (48), 19266-19269.

Specker, E., Book Review: Aspartic Acid Proteases as Therapeutic Targets. Edited by Arun K. Ghosh. ChemMedChem, 2011, 6 (6), 1130.

Anne V. Due, Jochen Kuper, Arie Geerlof, Jens Peter von Kries, and Matthias Wilmanns. Bi-substrate specificity in histidine/tryptophan biosynthesis isomerase from Mycobacterium tuberculosis by active site metamorphosis. PNAS, 2011, 108 (9), 3554-3559.

Waaler J, Machon O, von Kries JP, Wilson SR, Lundenes E, Wedlich D, Gradl D, Paulsen JE, Machonova O, Dembinski JL, Dinh H, Krauss S. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011, 71(1):197-205.

Bleif S, Hannemann F, Lisurek M, von Kries JP, Zapp J, Dietzen M, Antes I, Bernhardt R. Identification of CYP106A2 as a Regioselective Allylic Bacterial Diterpene Hydroxylase. Chembiochem, 2011, 12 (4), 576-582.

Christian F, Szaszák M, Friedl S, Drewianka S, Lorenz D, Goncalves A, Furkert J, Vargas C, Schmieder P, Götz F, Zühlke K, Moutty M, Göttert H, Joshi M, Reif B, Haase H, Morano I, Grossmann S, Klukovits A, Verli J, Gáspár R, Noack C, Bergmann M, Kass R, Hampel K, Kashin D, Genieser HG, Herberg FW, Willoughby D, Cooper DM, Baillie GS, Houslay MD, von Kries JP, Zimmermann B, Rosenthal W, Klussmann E. Small molecule AKAP-protein kinase A (PKA) interaction disruptors that activate PKA interfere with compartmentalized cAMP signaling in cardiac myocytes. J Biol Chem. 2011 Mar 18;286(11):9079-96.

von Kries JP, Warrier T, Podust LM. Identification of small-molecule scaffolds for p450 inhibitors. Curr Protoc Microbiol. 2010 Feb;Chapter 17:Unit17.4.

Johnsen L, Weigel C, von Kries JP, Møller M, Skarstad K. A novel DNA gyrase inhibitor rescues Escherichia coli dnaAcos mutant cells from lethal hyperinitiation. J Antimicrob Chemother. 2010 May;65(5):924-30. Epub 2010 Mar 12.

Choi, M., Eulenberg, C., Rolle, S., Kries, von, J.P., Luft, F.C., and Kettritz, R. (2010). The use of small molecule high-throughput screening to identify inhibitors of the proteinase 3-NB1 interaction. Clin. Exp. Immunol. 161, 389–396.

Lisurek, M., Rupp, B., Wichard, J., Neuenschwander, M., Kries, von, J.-P., Frank, R., Rademann, J., and Kühne, R. (2010). Design of chemical libraries with potentially bioactive molecules applying a maximum common substructure concept. Mol. Divers. 14, 401–408.

Kries, von, J.P., Warrier, T., and Podust, L.M. (2010). Identification of small-molecule scaffolds for p450 inhibitors. Curr Protoc Microbiol Chapter 17, Unit17.4–17.4.25.

The use of small molecule high-throughput screening to identify inhibitors of the proteinase 3-NB1 interaction, Clin. Exp.Immunol., 2010, 161, 389-396. Lisurek, M,  Rupp, B, Wichard, J,  Neuenschwander, M, von Kries, JP,  Frank, R, Rademann, J, Kühne, R, Molecular Diversity, 2009, 13, doi:10.1007/s11030-009-9187.

Podust, L.M., Ouellet, H., Kries, von, J.P., and de Montellano, P.R.O. (2009). Interaction of Mycobacterium tuberculosis CYP130 with heterocyclic arylamines. J. Biol. Chem. 284, 25211–25219.

Konkle, M.E., Hargrove, T.Y., Kleshchenko, Y.Y., Kries, von, J.P., Ridenour, W., Uddin, M.J., Caprioli, R.M., Marnett, L.J., Nes, W.D., Villalta, F., et al. (2009). Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase. J. Med. Chem. 52, 2846–2853.

Fetz, V., Knauer, S.K., Bier, C., Kries, von, J.-P., and Stauber, R.H. (2009). Translocation Biosensors - Cellular System Integrators to Dissect CRM1-Dependent Nuclear Export by Chemicogenomics. Sensors (Basel) 9, 5423–5445.

Podust, LM,  Ouellet, H, von Kries, JP, de Montellano, PO. Interaction of mycobacterium tuberculosis CYP130 with heterocyclic arylamines. J. Biol. Chem., 2009, 284, 25211-25219.

Konkle, ME, Hargrove, TY, Kleshchenko, YY, von Kries, JP, Ridenour, W, Uddin, MdJ, Caprioli, RM, Marnett, LJ, Nes, WD, Villalta, F, Waterman, MR and Lepesheva, GI. Indomethacin Amides as a Novel Molecular Scaffold for Targeting Trypanosoma cruzi Sterol 14alpha-Demethylase, J. Med. Chem., 2009, 52, 2846-2853. 

Nasser Eddine A, von Kries JP, Podust MV, Warrier T, Kaufmann SH, Podust LM. X-ray structure of 4,4'-dihydroxybenzophenone mimicking sterol substrate in the active site of sterol 14alpha -demethylase (CYP51),  J. Biol. Chem., 2008, 283, 15152-15159.

Hellmuth K, Grosskopf S, Lum CT, Würtele M, Röder N, von Kries JP, Rosario M, Rademann J and Birchmeier W. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-throughput Docking. PNAS, 2008, 105, 7275-7280.

Eddine, A.N., Kries, von, J.P., Podust, M.V., Warrier, T., Kaufmann, S.H.E., and Podust, L.M. (2008). X-ray structure of 4,4'-dihydroxybenzophenone mimicking sterol substrate in the active site of sterol 14alpha-demethylase (CYP51). J. Biol. Chem. 283, 15152–15159.

Podust, L.M., Kries, von, J.P., Eddine, A.N., Kim, Y., Yermalitskaya, L.V., Kuehne, R., Ouellet, H., Warrier, T., Alteköster, M., Lee, J.-S., et al. (2007). Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography. Antimicrob. Agents Chemother. 51, 3915–3923.

Mueller-Dieckmann C, Kernstock S, Lisurek M, von Kries JP, Haag F, Weiss MS, Koch-Nolte F. The structure of human ADP-ribosylhydrolase 3 (ARH3) provides insights into the reversibility of protein ADP-ribosylation. PNAS, 2006, 103, 15026-15031.

Eswaran J, von Kries JP, Marsden B, Longman E, Debreczeni JE, Ugochukwu E, Turnbull A, Lee WH, Knapp S, Barr AJ. Crystal structures and inhibitor identification for PTPN5, PTPRR and     PTPN7: a family of human MAPK-specific protein tyrosine phosphatases. Biochem J., 2006, 395, 483-491.  

Manger M, Scheck M, Prinz H, von Kries JP, Langer T, Saxena K, Schwalbe H, Fürstner A, Rademann J, Waldmann H. Discovery of Mycobacterium tuberculosis protein tyrosine phosphatase A (MptpA) inhibitors based on natural products and a fragment-based approach. ChemBioChem., 2005, 6, 1749-1753.

Podust LM, von Kries JP, Eddine AN, Kim Y, Yermalitskaya LV, Kuehne R, Ouellet H, Warrier T, Alteköster M, Lee JS, Rademann J, Oschkinat H, 

Singh RK, Kefala G, Janowski R, Mueller-Dieckmann C, von Kries JP, Weiss MS. The high-resolution Structure of LeuB (Rv2995c) from Mycobacterium tuberculosis. J. Mol. Biol., 2005 ,346, 1-11. 

von Kries JP, Winbeck G, Asbrand C, Schwarz-Romond T, Sochnikova N, Dell'Oro A, Behrens J, Birchmeier W. Hot spots in beta-catenin for interactions with LEF-1, conductin and APC.Nat Struct Biol., 2000, 7, 800-807.     

 

 

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