Small Molecules Drive Big Improvements in Immuno‐Oncology Therapies von Huck, Bayard R., Kötzner, Lisa, Urbahns, Klaus

Volltext

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases von Caldwell, Richard D, Qiu, Hui, Askew, Ben C, Bender, Andrew T, Brugger, Nadia, Camps, Montserrat, Dhanabal, Mohanraj, Dutt, Vikram, Eichhorn, Thomas, Gardberg, Anna S, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Healey, Brian, Hodous, Brian L, Huck, Bayard R, Johnson, Theresa L, Jones, Christopher, Jones, Reinaldo C, Mochalkin, Igor, Morandi, Federica, Nguyen, Ngan, Meyring, Michael, Potnick, Justin R, Santos, Dusica Cvetinovic, Schmidt, Ralf, Sherer, Brian, Shutes, Adam, Urbahns, Klaus, Follis, Ariele Viacava, Wegener, Ansgar A, Zimmerli, Simone C, Liu-Bujalski, Lesley

Volltext

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening von Czodrowski, Paul, Mallinger, Aurélie, Wienke, Dirk, Esdar, Christina, Pöschke, Oliver, Busch, Michael, Rohdich, Felix, Eccles, Suzanne A, Ortiz-Ruiz, Maria-Jesus, Schneider, Richard, Raynaud, Florence I, Clarke, Paul A, Musil, Djordje, Schwarz, Daniel, Dale, Trevor, Urbahns, Klaus, Blagg, Julian, Schiemann, Kai

Volltext

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases von Clarke, Paul A, Ortiz-Ruiz, Maria-Jesus, TePoele, Robert, Adeniji-Popoola, Olajumoke, Box, Gary, Court, Will, Czasch, Stephanie, El Bawab, Samer, Esdar, Christina, Ewan, Ken, Gowan, Sharon, De Haven Brandon, Alexis, Hewitt, Phillip, Hobbs, Stephen M, Kaufmann, Wolfgang, Mallinger, Aurélie, Raynaud, Florence, Roe, Toby, Rohdich, Felix, Schiemann, Kai, Simon, Stephanie, Schneider, Richard, Valenti, Melanie, Weigt, Stefan, Blagg, Julian, Blaukat, Andree, Dale, Trevor C, Eccles, Suzanne A, Hecht, Stefan, Urbahns, Klaus, Workman, Paul, Wienke, Dirk

Volltext

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore von Schiemann, Kai, Mallinger, Aurélie, Wienke, Dirk, Esdar, Christina, Poeschke, Oliver, Busch, Michael, Rohdich, Felix, Eccles, Suzanne A., Schneider, Richard, Raynaud, Florence I., Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Urbahns, Klaus, Blagg, Julian

Volltext

The expanding role for small molecules in immuno-oncology von Offringa, Rienk, Kötzner, Lisa, Huck, Bayard, Urbahns, Klaus

Volltext

Targeted Covalent Inhibitors for the Treatment of Malaria? von Kulkarni, Shashank, Urbahns, Klaus, Spangenberg, Thomas

Volltext

Crystalline Sponges as a Sensitive and Fast Method for Metabolite Identification: Application to Gemfibrozil and its Phase I and II Metabolites von Rosenberger, Lara, von Essen, Carolina, Khutia, Anupam, Kühn, Clemens, Urbahns, Klaus, Georgi, Katrin, Hartmann, Rolf W., Badolo, Lassina

Volltext

Stable and Storable N(CF3)2 Transfer Reagents von Schneider, Leon N., Tanzer Krauel, Eva‐Maria, Deutsch, Carl, Urbahns, Klaus, Bischof, Tobias, Maibom, Kristina A. M., Landmann, Johannes, Keppner, Fabian, Kerpen, Christoph, Hailmann, Michael, Zapf, Ludwig, Knuplez, Tanja, Bertermann, Rüdiger, Ignat'ev, Nikolai V., Finze, Maik

Volltext

Abstract 4198: Highly potent and selective DNA-PK inhibitor M3814 with sustainable anti-tumor activity in combination with radiotherapy von Fuchss, Thomas, Mederski, Werner W., Emde, Ulrich, Buchstallter, Hans-Peter, Zenke, Frank, Zimmermann, Astrid, Sirrenberg, Christian, Vassilev, Lubo, Damstrup, Lars, Urbahns, Klaus, Blaukat, Andree

Volltext

Overcoming Undesirable hERG Potency of Chemokine Receptor Antagonists Using Baseline Lipophilicity Relationships von Shamovsky, Igor, Connolly, Stephen, David, Laurent, Ivanova, Svetlana, Nordén, Bo, Springthorpe, Brian, Urbahns, Klaus

Volltext

Benzimidazole-5-sulfonamides as Novel Nonpeptide Luteinizing Hormone Releasing Hormone (LHRH) Antagonists: Minimization of Mechanism-Based CYP3A4 Inhibition von Hashimoto, Kentaro, Kataoka, Mikayo, Tatsuta, Miyuki, Yasoshima, Kayo, Yamamoto, Mako, Yura, Takeshi, Yamamoto, Noriyuki, Urbahns, Klaus, Gupta, Jang Bahadur, Li, Yingfu

Volltext

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19 von Mallinger, Aurélie, Schiemann, Kai, Rink, Christian, Sejberg, Jimmy, Honey, Mark A, Czodrowski, Paul, Stubbs, Mark, Poeschke, Oliver, Busch, Michael, Schneider, Richard, Schwarz, Daniel, Musil, Djordje, Burke, Rosemary, Urbahns, Klaus, Workman, Paul, Wienke, Dirk, Clarke, Paul A, Raynaud, Florence I, Eccles, Suzanne A, Esdar, Christina, Rohdich, Felix, Blagg, Julian

Volltext

Bis(trifluoromethyl)amido Complexes of Copper and Silver: Stable and storable N(CF3)2 transfer reagents von Schneider, Leon N, Tanzer Krauel, Eva-Maria, Deutsch, Carl, Urbahns, Klaus, Bischof, Tobias, Maibom, Kristina, Landmann, Johannes, Keppner, Fabian, Kerpen, Christoph, Hailmann, Michael, Zapf, Ludwig, Knuplez, Tanja, Bertermann, Rüdiger, Ignatiev, Nikolai V, Finze, Maik

Volltext

Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential von Clarke, Paul, Esdar, Christina, Mallinger, Aurelie, Schiemann, Kai, Waalboer, Dennis, Crumpler, Simon, Rink, Christian, Stieber, Frank, Calderini, Michel, Adeniji-Popoola, Olajumoke, Ortiz-Ruiz, Maria-Jesus, Samant, Rahul S., Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Schneider, Klaus, Busch, Michael, Stubbs, Mark, Burke, Rosemary, TePoele, Robert, Gowan, Sharon, Rohdich, Felix, Raynaud, Florence, Schneider, Richard, Poeschke, Oliver, Blaukat, Andree, Urbahns, Klaus, Workman, Paul, Kaufmann, Wolfgang, Simon, Stephanie, Eccles, Suzanne A., Dale, Trevor, Wienke, Dirk, Blagg, Julian

Volltext

Glycine amides as PPARα agonists von Urbahns, Klaus, Woltering, Michael, Nikolic, Susanne, Pernerstorfer, Josef, Bischoff, Hilmar, Dittrich-Wengenroth, Elke, Lustig, Klemens

Volltext

Selective intermediate-/small-conductance calcium-activated potassium channel (KCNN4) blockers are potent and effective therapeutics in experimental brain oedema and traumatic brai... von Mauler, Frank, Hinz, Volker, Horváth, Ervin, Schuhmacher, Joachim, Hofmann, Heiko A., Wirtz, Stephan, Hahn, Michael G., Urbahns, Klaus

Volltext

Tetrahydro-naphthols as orally available TRPV1 inhibitors von Urbahns, Klaus, Yura, Takeshi, Gupta, Jang B., Tajimi, Masaomi, Fujishima, Hiroshi, Masuda, Tsutomu, Yamamoto, Noriyuki, Ikegami, Yuka, Marumo, Makiko, Yasoshima, Kayo, Yoshida, Nagahiro, Moriwaki, Toshiya, Madge, David, Chan, Fiona, Mogi, Muneto

Volltext

Glycine amides as PPARa agonists von Urbahns, Klaus, Woltering, Michael, Nikolic, Susanne, Pernerstorfer, Josef, Bischoff, Hilmar, Dittrich-Wengenroth, Elke, Lustig, Klemens

Volltext

Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites von Shamovsky, Igor, de Graaf, Chris, Alderin, Lisa, Bengtsson, Malena, Bladh, Håkan, Börjesson, Lena, Connolly, Stephen, Dyke, Hazel J, van den Heuvel, Marco, Johansson, Henrik, Josefsson, Bo-Göran, Kristoffersson, Anna, Linnanen, Tero, Lisius, Annea, Männikkö, Roope, Nordén, Bo, Price, Steve, Ripa, Lena, Rognan, Didier, Rosendahl, Alexander, Skrinjar, Marco, Urbahns, Klaus

Volltext