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Start Over Author "Schonbrunn A" Journal journal of medicinal chemistry
7 results on '"Schonbrunn A"'

1. Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor

Author

Divakaran, Anand, primary, Talluri, Siva K., additional, Ayoub, Alex M., additional, Mishra, Neeraj K., additional, Cui, Huarui, additional, Widen, John C., additional, Berndt, Norbert, additional, Zhu, Jin-Yi, additional, Carlson, Angela S., additional, Topczewski, Joseph J., additional, Schonbrunn, Ernst K., additional, Harki, Daniel A., additional, and Pomerantz, William C. K., additional

Published
2018
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2. Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases

Author

Schonbrunn, Ernst, primary, Betzi, Stephane, additional, Alam, Riazul, additional, Martin, Mathew P., additional, Becker, Andreas, additional, Han, Huijong, additional, Francis, Rawle, additional, Chakrasali, Ramappa, additional, Jakkaraj, Sudhakar, additional, Kazi, Aslamuzzaman, additional, Sebti, Said M., additional, Cubitt, Christopher L., additional, Gebhard, Anthony W., additional, Hazlehurst, Lori A., additional, Tash, Joseph S., additional, and Georg, Gunda I., additional

Published
2013
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3. Development of o-Chlorophenyl Substituted Pyrimidines as Exceptionally Potent Aurora Kinase Inhibitors

Author

Lawrence, Harshani R., primary, Martin, Mathew P., additional, Luo, Yunting, additional, Pireddu, Roberta, additional, Yang, Hua, additional, Gevariya, Harsukh, additional, Ozcan, Sevil, additional, Zhu, Jin-Yi, additional, Kendig, Robert, additional, Rodriguez, Mercedes, additional, Elias, Roy, additional, Cheng, Jin Q., additional, Sebti, Saïd M., additional, Schonbrunn, Ernst, additional, and Lawrence, Nicholas J., additional

Published
2012
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4. Fragment-Based and Structure-Guided Discovery and Optimization of Rho Kinase Inhibitors

Author

Li, Rongshi, primary, Martin, Mathew P., additional, Liu, Yan, additional, Wang, Binglin, additional, Patel, Ronil A., additional, Zhu, Jin-Yi, additional, Sun, Nan, additional, Pireddu, Roberta, additional, Lawrence, Nicholas J., additional, Li, Jiannong, additional, Haura, Eric B., additional, Sung, Shen-Shu, additional, Guida, Wayne C., additional, Schonbrunn, Ernst, additional, and Sebti, Said M., additional

Published
2012
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5. Developmentof Highly Potent and Selective DiaminothiazoleInhibitors of Cyclin-Dependent Kinases.

Author

Schonbrunn, Ernst, Betzi, Stephane, Alam, Riazul, Martin, Mathew P., Becker, Andreas, Han, Huijong, Francis, Rawle, Chakrasali, Ramappa, Jakkaraj, Sudhakar, Kazi, Aslamuzzaman, Sebti, Said M., Cubitt, Christopher L., Gebhard, Anthony W., Hazlehurst, Lori A., Tash, Joseph S., and Georg, Gunda I.

Subjects
*CYCLIN-dependent kinase inhibitors, *THIAZOLES, *CELL cycle regulation, *THREONINE, *LIGAND binding (Biochemistry), *CANCER cell proliferation, *STATISTICAL correlation, *RETINOBLASTOMA
Abstract

Cyclin-dependent kinases (CDKs) areserine/threonine protein kinasesthat act as key regulatory elements in cell cycle progression. Wedescribe the development of highly potent diaminothiazole inhibitorsof CDK2 (IC50= 0.0009–0.0015 μM) from a singlehit compound with weak inhibitory activity (IC50= 15 μM),discovered by high-throughput screening. Structure-based design wasperformed using 35 cocrystal structures of CDK2 liganded with distinctanalogues of the parent compound. The profiling of compound 51against a panel of 339 kinases revealed high selectivityfor CDKs, with preference for CDK2 and CDK5 over CDK9, CDK1, CDK4,and CDK6. Compound 51inhibited the proliferation of13 out of 15 cancer cell lines with IC50values between0.27 and 6.9 μM, which correlated with the complete suppressionof retinoblastoma phosphorylation and the onset of apoptosis. Combined,the results demonstrate the potential of this new inhibitors seriesfor further development into CDK-specific chemical probes or therapeutics. [ABSTRACT FROM AUTHOR]

Published
2013
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