2017
Na+ entry through heteromeric TRPC4/C1 channels mediates (-)Englerin A-induced cytotoxicity in synovial sarcoma cellsMuraki K, Ohnishi K, Takezawa A, Suzuki H, Hatano N, Muraki Y, Hamzah N, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon R S, Beech D J. Scientific Reports. 2017; 7 (1): doi: 10.1038/s41598-017-17303-3
Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of CancerLucking U, Scholz A, Lienau P, Siemeister G, Kosemund D, Bohlmann R, Briem H, Terebesi I, Meyer K, Prelle K, Denner K, Bomer U, Schafer M, Eis K, Valencia R, Ince S, von Nussbaum F, Mumberg D, Ziegelbauer K, Klebl B, Choidas A, Nussbaumer P, Baumann M, Schultz-Fademrecht C, Ruhter G, Eickhoff J, Brands M. ChemMedChem. 2017; 12 (21): 1776-1793. doi: 10.1002/cmdc.201700447
Discovery of a Novel Inhibitor of the Hedgehog Signaling Pathway through Cell-Based Compound Discovery and Target PredictionKremer L, Schultz-Fademrecht C, Baumann M, Habenberger P, Choidas A, Klebl B, Kordes S, Scholer H R, Sterneckert J, Ziegler S, Schneider G, Waldmann H. Angew Chem Int Ed Engl. 2017; 56 (42): 13021-13025. doi: 10.1002/anie.201707394
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor ReceptorEngel J, Smith S, Lategahn J, Tumbrink H L, Goebel L, Becker C, Hennes E, Keul M, Unger A, Muller H, Baumann M, Schultz-Fademrecht C, Gunther G, Hengstler J G, Rauh D. J Med Chem. 2017; 60 (18): 7725-7744. doi: 10.1021/acs.jmedchem.7b00515
Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinomaBragelmann J, Dammert M A, Dietlein F, Heuckmann J M, Choidas A, Bohm S, Richters A, Basu D, Tischler V, Lorenz C, Habenberger P, Fang Z, Ortiz-Cuaran S, Leenders F, Eickhoff J, Koch U, Getlik M, Termathe M, Sallouh M, Greff Z, Varga Z, Balke-Want H, French C A, Peifer M, Reinhardt H C, Orfi L, Keri G, Ansen S, Heukamp L C, Buttner R, Rauh D, Klebl B M, Thomas R K, Sos M L. Cell Rep. 2017; 20 (12): 2833-2845. doi: 10.1016/j.celrep.2017.08.082
Stabilization of protein-protein interactions in drug discoverySijbesma E, Skora L, Leysen S, Brunsveld L, Koch U, Nussbaumer P, Jahnke W, Ottmann C. Biochemistry. 2017; 56 (30): 3972-3982. doi: 10.1021/acs.biochem.7b00153
Identification of Two Secondary Ligand Binding Sites in 14-3-3 Proteins Using Fragment ScreeningSijbesma E, Skora L, Leysen S, Brunsveld L, Koch U, Nussbaumer P, Jahnke W, Ottmann C. Biochemistry. 2017; 56 (30): 3972-3982. doi: 10.1021/acs.biochem.7b00153
Small-Molecule Inhibition of the UNC119-Cargo InteractionMejuch T, Garivet G, Hofer W, Kaiser N, Fansa E K, Ehrt C, Koch O, Baumann M, Ziegler S, Wittinghofer A, Waldmann H. Angew Chem Int Ed Engl. 2017; 56 (22): 6181-6186. doi: 10.1002/anie.201701905
Covalent Protein Labeling at Glutamic AcidsMartin-Gago P, Fansa E K, Winzker M, Murarka S, Janning P, Schultz-Fademrecht C, Baumann M, Wittinghofer A, Waldmann H. Cell Chem Biol. 2017; 24 (5): 589-597 e585. doi: 10.1016/j.chembiol.2017.03.015
ATM Kinase Inhibitors: HTS Cellular Imaging Assay Using Cellomics™ ArrayScan VTI PlatformBardelle C, Boros J. Methods Mol Biol. 2017; 1599 57-70. doi: 10.1007/978-1-4939-6955-5_5
An Adaptable High-Throughput Technology Enabling the Identification of Specific Transcription ModulatorsBergbrede T, Hoberg E, Larsson N G, Falkenberg M, Gustafsson C M. SLAS Discov. 2017; 22 (4): 378-386. doi: 10.1177/2472555217690326
Picomolar, selective and subtype specific small-molecule inhibition of TRPC1/4/5 channelsRubaiy H N, Ludlow M J, Henrot M, Gaunt H J, Miteva K, Cheung S Y, Tanahashi Y, Hamzah N, Musialowski K E, Blythe N M, Appleby H L, Bailey M A, McKeown L, Taylor R, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon R S, Muraki K, Beech D J. J Biol Chem. 2017; 292 (20): 8158-8173. doi: 10.1074/jbc.M116.773556
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor ReceptorTomassi S, Lategahn J, Engel J, Keul M, Tumbrink H L, Ketzer J, Muhlenberg T, Baumann M, Schultz-Fademrecht C, Bauer S, Rauh D. J Med Chem. 2017; 60 (6): 2361-2372. doi: 10.1021/acs.jmedchem.6b01626
A PDE6d-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2Martin-Gago P, Fansa E K, Klein C H, Murarka S, Janning P, Schurmann M, Metz M, Ismail S, Schultz-Fademrecht C, Baumann M, Bastiaens P I, Wittinghofer A, Waldmann H. Angew Chem Int Ed Engl. 2017; 56 (9): 2423-2428. doi: 10.1002/anie.201610957
New insights into the intracellular distribution pattern of cationic amphiphilic drugsVater M, Mockl L, Gormanns V, Schultz Fademrecht C, Mallmann A M, Ziegart-Sadowska K, Zaba M, Frevert M L, Brauchle C, Holsboer F, Rein T, Schmidt U, Kirmeier T. Sci Rep. 2017; 7 44277. doi: 10.1038/srep44277
Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding SiteMurarka S, Martin-Gago P, Schultz-Fademrecht C, Al Saabi A, Baumann M, Fansa E K, Ismail S, Nussbaumer P, Wittinghofer A, Waldmann H. Chemistry. 2017; 23 (25): 6083-6093. doi: 10.1002/chem.201603222
