Browse by Research Team

2023

The FGFR inhibitor PD173074 binds to the C-terminus of oncofetal HMGA2 and modulates its DNA-binding and transcriptional activation functions.
Ahmed, S.M., Ragunathan, P., Shin, J., Peter, S., Kleissle, S., Neuenschwander, M., Schäfer, R., von Kries, J.P., Grüber, G. and Dröge, P.
FEBS Letters 597 (15): 1977-1988. August 2023

2021

Design and synthesis of novel fluorescently labeled analogs of vemurafenib targeting MKK4.
Kircher, T., Pantsar, T., Oder, A., von Kries, J.P., Juchum, M., Pfaffenrot, B., Kloevekorn, P., Albrecht, W., Selig, R. and Laufer, S.
European Journal of Medicinal Chemistry 2019 : 112901. 1 January 2021

Natural compounds and synthetic drugs to target type-2 cannabinoid (CB(2)) receptor.
Guba, W., Nazaré, M. and Grether, U.
In: New tools to interrogate endocannabinoid signalling : from natural compounds to synthetic drugs. RSC Drug Discovery Series, 76 . Royal Society of Chemistry, Croydon, 89-167. ISBN 978-1-78801-801-2 2021

2020

From pyrazolones to azaindoles: evolution of active-site SHP2 inhibitors based on scaffold hopping and bioisosteric replacement.
Mostinski, Y., Heynen, G.J.J.E., López-Alberca, M.P., Paul, J., Miksche, S., Radetzki, S., Schaller, D., Shanina, E., Seyffarth, C., Kolomeets, Y., Ziebart, N., de Schryver, J., Oestreich, S., Neuenschwander, M., Roske, Y., Heinemann, U., Rademacher, C., Volkamer, A., von Kries, J.P., Birchmeier, W. and Nazaré, M.
Journal of Medicinal Chemistry 63 (23): 14780-14804. 10 December 2020

Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells.
Barone, M., Müller, M., Chiha, S., Ren, J., Albat, D., Soicke, A., Dohmen, S., Klein, M., Bruns, J., van Dinther, M., Opitz, R., Lindemann, P., Beerbaum, M., Motzny, K., Roske, Y., Schmieder, P., Volkmer, R., Nazaré, M., Heinemann, U., Oschkinat, H., Ten Dijke, P., Schmalz, H.G. and Kühne, R.
Proceedings of the National Academy of Sciences of the United States of America 117 (47): 29684-29690. 24 November 2020

Diverse chemotypes drive biased signaling by cannabinoid receptors.
Miljuš, T., Heydenreich, F.M., Gazzi, T., Kimbara, A., Rogers-Evans, M., Nettekoven, M., Zirwes, E., Osterwald, A., Rufer, A.C., Ullmer, C., Guba, W., Le Gouill, C., Fingerle, J., Nazaré, M., Grether, U., Bouvier, M. and Veprintsev, D.B.
bioRxiv : 2020.11.09.375162. 10 November 2020

NMR quality control of fragment libraries for screening.
Sreeramulu, S., Richter, C., Kuehn, T., Azzaoui, K., Blommers, M.J.J., Del Conte, R., Fragai, M., Trieloff, N., Schmieder, P., Nazaré, M., Specker, E., Ivanov, V., Oschkinat, H., Banci, L. and Schwalbe, H.
Journal of Biomolecular NMR 74 (10-11): 555-563. November 2020

Development of high-specificity fluorescent probes to enable cannabinoid type 2 receptor studies in living cells.
Sarott, R.C., Westphal, M., Pfaff, P., Korn, C., Sykes, D.A., Gazzi, T., Brennecke, B., Atz, K., Weise, M., Mostinski, Y., Hompluem, P., Koers, E., Miljus, T., Roth, N.J., Asmelash, H., Vong, M.C., Piovesan, J., Guba, W., Rufer, A., Kusznir, E.A., Huber, S., Raposo, C., Zirwes, E.A., Osterwald, A., Pavlovic, A., Moes, S., Beck, J., Benito-Cuesta, I., Grande, T., Ruiz de Martin, S., Yeliseev, A.A., Drawnel, F., Widmer, G., Holzer, D., van der Wel, T., Mandhair, H., Yuan, C.Y., Drobyski, W., Saroz, Y., Grimsey, N.L., Honer, M., Fingerle, J., Gawrisch, K., Romero, J., Hillard, C., Varga, Z., van der Stelt, M., Pacher, P., Gertsch, J., McCormick, P., Ullmer, C., Oddi, S., Maccarrone, M., Veprintsev, D., Nazaré, M., Grether, U. and Carreira, E.M.
Journal of the American Chemical Society 142 (40): 16953-16964. 7 October 2020

A palladium-catalyzed domino reaction to access 3-amino-2H-indazoles from hydrazines and 2-halobenzonitriles.
Alsalim, R., Lindemann, P., López-Alberca, M.P., Miksche, S., Czechtizky, W., Halland, N. and Nazaré, M.
Organic Letters 22 (18): 7393-7396. 18 September 2020

A semi-automated intestinal organoid screening method demonstrates epigenetic control of epithelial maturation.
Ostrop, J., Zwiggelaar, R., Pedersen, M.T., Gerbe, F., Bösl, K., Lindholm, H.T., Díez-Sánchez, Al., Parmar, N., Radetzki, S., von Kries, J.P., Jay, P., Jensen, K.B., Arrowsmith, C. and Oudhoff, M.J.
bioRxiv : 2020.07.23.217414. 24 July 2020

Preclinical lead optimization of a 1,2,4-triazole based tankyrase inhibitor.
Waaler, J., Leenders, R., Sowa, S.T., Alam Brinch, S., Lycke, M., Nieczypor, P., Aertssen, S., Murthy, S., Galera-Prat, A., Damen, E., Wegert, A., Nazare, M., Lehtiö, L. and Krauss, S.
Journal of Medicinal Chemistry 63 (13): 6834-6846. 9 July 2020

Revealing cytotoxic substructures in molecules using deep learning.
Webel, H.E., Kimber, T.B., Radetzki, S., Neuenschwander, M., Nazaré, M. and Volkamer, A.
Journal of Computer-Aided Molecular Design 34 (7): 731-746. July 2020

Dual-mode detection of bacterial 16S ribosomal RNA in tissues.
Xu, S., Zhang, Q., Han, X., Wang, Y., Wang, X., Nazaré, M., Jiang, J.D. and Hu, H.Y.
ACS Sensors 5 (6): 1650-1656. 26 June 2020

Monensin, a novel potent MYB inhibitor, suppresses proliferation of acute myeloid leukemia and adenoid cystic carcinoma cells.
Yusenko, M.V., Trentmann, A., Andersson, M.K., Ghani, L.A., Jakobs, A., Arteaga Paz, M.F., Mikesch, J.H., von Kries, J.P., Stenman, G. and Klempnauer, K.H.
Cancer Letters 479 : 61-70. 1 June 2020

An activatable lanthanide luminescent probe for time-gated detection of nitroreductase in live bacteria.
Brennecke, B., Wang, Q., Zhang, Q., Hu, H.Y. and Nazaré, M.
Angewandte Chemie International Edition 59 (22): 8512-8516. 25 May 2020

Cyclin-dependent kinase 18 controls trafficking of aquaporin-2 and its abundance through ubiquitin ligase STUB1, which functions as an AKAP.
Dema, A., Faust, D., Lazarow, K., Wippich, M., Neuenschwander, M., Zühlke, K., Geelhaar, A., Pallien, T., Hallscheidt, E., Eichhorst, J., Wiesner, B., Cernecká, H., Popp, O., Mertins, P., Dittmar, G., von Kries, J.P. and Klussmann, E.
Cells 9 (3): 673. 10 March 2020

2019

Small-molecule lysophosphatidic acid receptor 5 (LPAR5) antagonists: versatile pharmacological tools to regulate inflammatory signaling in BV-2 microglia cells.
Plastira, I., Joshi, L., Bernhart, E., Schoene, J., Specker, E., Nazare, M. and Sattler, W.
Frontiers in Cellular Neuroscience 13 : 531. 29 December 2019

Probing 2H-indazoles as template for SGK1, Tie2 and SRC kinase inhibitors.
Schoene, J., Gazzi, T., Lindemann, P., Christmann, M., Volkamer, A. and Nazaré, M.
ChemMedChem 14 (16): 1514-1527. 20 August 2019

Regulation of influenza a virus mRNA splicing by CLK1.
Artarini, A., Meyer, M., Shin, Y.J., Huber, K., Hilz, N., Bracher, F., Eros, D., Orfi, L., Keri, G., Goedert, S., Neuenschwander, M., von Kries, J., Domovich-Eisenberg, Y., Dekel, N., Szabadkai, I., Lebendiker, M., Horváth, Z., Danieli, T., Livnah, O., Moncorgé, O., Frise, R., Barclay, W., Meyer, T.F. and Karlas, A.
Antiviral Research 168 : 187-196. August 2019

Identification of TMEM206 proteins as pore of PAORAC/ASOR acid-sensitive chloride channels.
Ullrich, F., Blin, S., Lazarow, K., Daubitz, T., von Kries, J.P. and Jentsch, T.J.
eLife 8 : e49187. 18 July 2019

Vinylphosphonites for staudinger-induced chemoselective peptide cyclization and functionalization.
Kasper, M.A, Glanz, M., Oder, A., Schmieder, P., von Kries, J.P. and Hackenberger, C.P.R.
Chemical Science 10 (25): 6322-6329. 7 July 2019

High-throughput screening for modulators of CFTR activity based on genetically engineered cystic fibrosis disease-specific iPSCs.
Merkert, S., Schubert, M., Olmer, R., Engels, L., Radetzki, S., Veltman, M., Scholte, B.J., Zöllner, J., Pedemonte, N., Galietta, L.J.V., von Kries, J.P. and Martin, U.
Stem Cell Reports 12 (6): 1389-1403. 11 June 2019

Rapid synthesis of γ-halide/pseudohalide-substituted cyanine sensors with programmed generation of singlet oxygen.
Zhang, Q., Xu, S., Lai, F., Wang, Y., Zhang, N., Nazare, M. and Hu, H.Y.
Organic Letters 21 (7): 2121-2125. 5 April 2019

EU-OPENSCREEN: a novel collaborative approach to facilitate chemical biology.
Brennecke, P., Rasina, D., Aubi, O., Herzog, K., Landskron, J., Cautain, B., Vicente, F., Quintana, J., Mestres, J., Stechmann, B., Ellinger, B., Brea, J., Kolanowski, J.L., Pilarski, R., Orzaez, M., Pineda-Lucena, A., Laraia, L., Nami, F., Zielenkiewicz, P., Paruch, K., Hansen, E., von Kries, J.P., Neuenschwander, M., Specker, E., Bartunek, P., Simova, S., Leśnikowski, Z., Krauss, S., Lehtiö, L., Bilitewski, U., Brönstrup, M., Taskén, K., Jirgensons, A., Lickert, H., Clausen, M.H., Andersen, J.H., Vicent, M.J., Genilloud, O., Martinez, A., Nazaré, M., Fecke, W. and Gribbon, P.
SLAS Discovery 24 (3): 398-413. 1 March 2019

A pharmacological master key mechanism that unlocks the selectivity filter gate in K(+) channels.
Schewe, M., Sun, H., Mert, Ü., Mackenzie, A., Pike, A.C.W., Schulz, F., Constantin, C., Vowinkel, K.S., Conrad, L.J., Kiper, A.K., Gonzalez, W., Musinszki, M., Tegtmeier, M., Pryde, D.C., Belabed, H., Nazare, M., de Groot, B.L., Decher, N., Fakler, B., Carpenter, E.P., Tucker, S.J. and Baukrowitz, T.
Science 363 (6429): 875-880. 22 February 2019

A new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy.
Marcinkowski, P., Hoyer, I., Specker, E., Furkert, J., Rutz, C., Neuenschwander, M., Sobottka, S., Sun, H., Nazare, M., Berchner-Pfannschmidt, U., von Kries, J.P., Eckstein, A., Schülein, R. and Krause, G.
Thyroid 29 (1): 111-123. 23 January 2019

2018

Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway.
Klein, W., Rutz, C., Eckhard, J., Provinciael, B., Specker, E., Neuenschwander, M., Kleinau, G., Scheerer, P., von Kries, J.P., Nazaré, M., Vermeire, K. and Schülein, R.
PLoS ONE 13 (12): e0208641. 13 December 2018

CellFy: a cell-based fragment screen against C-type lectins.
Schulze, J., Baukmann, H., Wawrzinek, R., Fuchsberger, F., Specker, E., Aretz, J., Nazaré, M. and Rademacher, C.
ACS Chemical Biology 13 (12): 3229-3235. December 2018

Allosteric inhibition of a mammalian lectin.
Aretz, J., Anumala, U.R., Fuchsberger, F.F., Molavi, N., Ziebart, N., Zhang, H., Nazaré, M. and Rademacher, C.
Journal of the American Chemical Society 140 (44): 14915-14925. 7 November 2018

Systematic pharmacological screens uncover novel pathways involved in cerebral cavernous malformations.
Otten, C., Knox, J., Boulday, G., Eymery, M., Haniszewski, M., Neuenschwander, M., Radetzki, S., Vogt, I., Hähn, K., De Luca, C., Cardoso, C., Hamad, S., Igual Gil, C., Roy, P., Albiges‐Rizo, C., Faurobert, E., von Kries, J.P., Campillos, M., Tournier‐Lasserve, E., Derry, W.B. and Abdelilah-Seyfried, S.
EMBO Molecular Medicine 10 (10): e9155. 1 October 2018

In vivo imaging of MMP-13 activity using a specific polymer-FRET peptide conjugate detects early osteoarthritis and inhibitor efficacy.
Duro-Castano, A., Lim, N.H., Tranchant, I., Amoura, M., Beau, F., Wieland, H., Kingler, O., Herrmann, M., Nazaré, M., Plettenburg, O., Dive, V., Vicent, M.J. and Nagase, H.
Advanced Functional Materials 28 (37): 1802738. 12 September 2018

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.
Ruess, D.A., Heynen, G.J., Ciecielski, K.J., Ai, J., Berninger, A., Kabacaoglu, D., Görgülü, K., Dantes, Z., Wörmann, S.M., Diakopoulos, K.N., Karpathaki, A.F., Kowalska, M., Kaya-Aksoy, E., Song, L., Zeeuw van der Laan, E.A., López-Alberca, M.P., Nazaré, M., Reichert, M., Saur, D., Erkan, M.M., Hopt, U.T., Sainz, B., Birchmeier, W., Schmid, R.M., Lesina, M. and Algül, H.
Nature Medicine 24 (7): 954-960. July 2018

A general one-pot synthesis of 2H-indazoles using an organophosphorus-silane system.
Schoene, J., Bel Abed, H., Schmieder, P., Christmann, M. and Nazaré, M.
Chemistry - A European Journal 24 (36): 9090-9100. 26 June 2018

Drug discovery with an RBM20 dependent titin splice reporter identifies cardenolides as lead structures to improve cardiac filling.
Liss, M., Radke, M.H., Eckhard, J., Neuenschwander, M., Dauksaite, V., von Kries, J.P. and Gotthardt, M.
PLoS ONE 13 (6): e0198492. 11 June 2018

Novel strategy for the preparation of 3-perfluoroalkylated-2 H-indazole derivatives.
Bel Abed, H., Weißing, N., Schoene, J., Paulus, J., Sewald, N. and Nazaré, M.
Tetrahedron Letters 59 (19): 1813-1815. 9 May 2018

A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging.
Liu, Y., Zhang, L., Nazare, M., Yao, Q. and Hu, H.Y.
Acta Pharmaceutica Sinica B 8 (3): 401-408. May 2018

Loss-of-function uORF mutations in human malignancies.
Schulz, J., Mah, N., Neuenschwander, M., Kischka, T., Ratei, R., Schlag, P.M., Castaños-Vélez, E., Fichtner, I., Tunn, P.U., Denkert, C., Klaas, O., Berdel, W.E., von Kries, J.P., Makalowski, W., Andrade-Navarro, M.A., Leutz, A. and Wethmar, K.
Scientific Reports 8 (1): 2395. 5 February 2018

An AKAP-Lbc-RhoA interaction inhibitor promotes the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells.
Schrade, K., Tröger, J., Eldahshan, A., Zühlke, K., Abdul Azeez, K.R., Elkins, J.M., Neuenschwander, M., Oder, A., Elkewedi, M.M.H., Jaksch, S., Andrae, K., Li, J., Fernandes, J., Müller, P.M., Grunwald, S., Marino, S.F., Vukićević, T., Eichhorst, J., Wiesner, B., Weber, M., Kapiloff, M., Rocks, O., Daumke, O., Wieland, T., Knapp, S., von Kries, J.P. and Klussmann, E.
PLoS ONE 13 (1): e0191423. 26 January 2018

Identification and characterization of a single high-affinity fatty acid binding site in human serum albumin.
Wenskowsky, L., Schreuder, H., Derdau, V., Matter, H., Volkmar, J., Nazaré, M., Opatz, T. and Petry, S.
Angewandte Chemie International Edition 57 (4): 1044-1048. 22 January 2018

2017

Discovery of a novel series of tankyrase inhibitors by a hybridization approach.
Anumala, U.R., Waaler, J., Nkizinkiko, Y., Ignatev, A., Lazarow, K., Lindemann, P., Olsen, P.A., Murthy, S., Obaji, E., Majouga, A.G., Leonov, S., von Kries, J.P., Lehtiö, L., Krauss, S. and Nazaré, M.
Journal of Medicinal Chemistry 60 (24): 10013-10025. 28 December 2017

A chemical disruptor of the ClpX chaperone complex attenuates the virulence of multidrug-resistant Staphylococcus aureus.
Fetzer, C., Korotkov, V.S., Thänert, R., Lee, K.M., Neuenschwander, M., von Kries, J.P., Medina, E. and Sieber, S.A.
Angewandte Chemie International Edition 56 (49): 15746-15750. 4 December 2017

Identification of a novel benzimidazole pyrazolone scaffold that inhibits KDM4 lysine demethylases and reduces proliferation of prostate cancer cells.
Carter, D.M., Specker, E., Przygodda, J., Neuenschwander, M., von Kries, J.P., Heinemann, U., Nazaré, M. and Gohlke, U.
SLAS Discovery 22 (7): 801-812. 1 August 2017

Small molecules targeting human N-acetylmannosamine kinase.
Hinderlich, S., Neuenschwander, M., Wratil, P.R., Oder, A., Lisurek, M., Nguyen, L.D., von Kries, J.P. and Hackenberger, C.P.R.
ChemBioChem 18 (13): 1279-1285. 4 July 2017

Neuronal chemosensation and osmotic stress response converge in the regulation of aqp-8 in C. elegans.
Igual Gil, C., Jarius, M., von Kries, J.P. and Rohlfing, A.K.
Frontiers in Physiology 8 : 380. 9 June 2017

Direct experimental evidence for halogen-aryl π interactions in solution from molecular torsion balances.
Sun, H., Horatscheck, A., Martos, V., Bartetzko, M., Uhrig, U., Lentz, D., Schmieder, P. and Nazaré, M.
Angewandte Chemie International Edition 56 (23): 6454-6458. 1 June 2017

Statin and rottlerin small-molecule inhibitors restrict colon cancer progression and metastasis via MACC1.
Juneja, M., Kobelt, D., Walther, W., Voss, C., Smith, J., Specker, E., Neuenschwander, M., Gohlke, B.O., Dahlmann, M., Radetzki, S., Preissner, R., von Kries, J.P., Schlag, P.M. and Stein, U.
PLoS Biology 15 (6): e2000784. 1 June 2017

A straightforward approach to N-substituted-2 H-indazol-2-amines through reductive cyclization.
Schoene, J., Bel Abed, H., Christmann, M. and Nazare, M.
Tetrahedron Letters 58 (16): 1633-1635. 19 April 2017

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

Pharmacological restoration and therapeutic targeting of the B-cell phenotype in classical Hodgkin's lymphoma.
Du, J., Neuenschwander, M., Yu, Y., Däbritz, J.H.M., Neuendorff, N.R., 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, J.P., Lee, S. and Schmitt, C.A.
Blood 129 (1): 71-81. 5 January 2017

2016

Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles.
Bel Abed, H., Schoene, J., Christmann, M. and Nazare, M.
Organic & Biomolecular Chemistry 14 (36): 8520-8528. 28 September 2016