Publications | Lead Discovery Center

2017

Na+ entry through heteromeric TRPC4/C1 channels mediates (-)Englerin A-induced cytotoxicity in synovial sarcoma cells

Muraki 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 Cancer

Lucking 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 Prediction

Kremer 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 Receptor

Engel 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 carcinoma

Bragelmann 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 discovery

Sijbesma 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 Screening

Sijbesma 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 Interaction

Mejuch 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 Acids

Martin-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 Platform

Bardelle 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 Modulators

Bergbrede 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 channels

Rubaiy 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 Receptor

Tomassi 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 Arl2

Martin-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 drugs

Vater 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 Site

Murarka 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

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