Structure;#8208;Based Design of Selective Noncovalent CDK12 Inhibitors

Johannes, Jeffrey W.; Denz, Christopher R.; Su, Nancy; Wu, Allan; Impastato, Anna C.; Mlynarski, Scott; Varnes, Jeffrey G.; Prince, D. Bryan; Cidado, Justin; Gao, Ning; Haddrick, Malcolm; Jones, Natalie H.; Li, Shaobin; Li, Xiuwei; Liu, Yang; Nguyen, Toan B.; O,; Connell, Nichole; Rivers, Emma; Robbins, Daniel W.; Tomlinson, Ronald; Yao, Tieguang; Zhu, Xiahui; Ferguson, Andrew D.; Lamb, Michelle L.; Manchester, John I.; Guichard, Sylvie

doi:10.1002/cmdc.201700695

Title: Structure;#8208;Based Design of Selective Noncovalent CDK12 Inhibitors

Journal Article · Fri May 24 00:00:00 EDT 2019 · ChemMedChem

DOI:https://doi.org/10.1002/cmdc.201700695· OSTI ID:1523525

Johannes, Jeffrey W.; Denz, Christopher R.; Su, Nancy; Wu, Allan; Impastato, Anna C.; Mlynarski, Scott; Varnes, Jeffrey G.; Prince, D. Bryan; Cidado, Justin; Gao, Ning; Haddrick, Malcolm; Jones, Natalie H.; Li, Shaobin; Li, Xiuwei; Liu, Yang; Nguyen, Toan B.; O,; Connell, Nichole; Rivers, Emma; Robbins, Daniel W. more »

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Research Organization:: Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)

Sponsoring Organization:: INDUSTRY

OSTI ID:: 1523525

Journal Information:: ChemMedChem, Vol. 13, Issue (3) ; 02, 2018

Country of Publication:: United States

Language:: ENGLISH

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Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties Bibian, Mathieu; Rahaim, Ronald J.; Choi, Jun Yong Bioorganic & Medicinal Chemistry Letters, Vol. 23, Issue 15 https://doi.org/10.1016/j.bmcl.2013.05.075	journal	August 2013
Ovarian carcinoma CDK12 mutations misregulate expression of DNA repair genes via deficient formation and function of the Cdk12/CycK complex Ekumi, Kingsley M.; Paculova, Hana; Lenasi, Tina Nucleic Acids Research, Vol. 43, Issue 5 https://doi.org/10.1093/nar/gkv101	journal	February 2015
Cyclin K goes with Cdk12 and Cdk13 Kohoutek, Jiri; Blazek, Dalibor Cell Division, Vol. 7, Issue 1 https://doi.org/10.1186/1747-1028-7-12	journal	January 2012
Structures of the CDK12/CycK complex with AMP-PNP reveal a flexible C-terminal kinase extension important for ATP binding Dixon-Clarke, Sarah E.; Elkins, Jonathan M.; Cheng, S. -W. Grace Scientific Reports, Vol. 5, Issue 1 https://doi.org/10.1038/srep17122	journal	November 2015
The structure and substrate specificity of human Cdk12/Cyclin K Bösken, Christian A.; Farnung, Lucas; Hintermair, Corinna Nature Communications, Vol. 5, Issue 1 https://doi.org/10.1038/ncomms4505	journal	March 2014
Laying a trap to kill cancer cells: PARP inhibitors and their mechanisms of action Pommier, Y.; OConnor, M. J.; de Bono, J. Science Translational Medicine, Vol. 8, Issue 362 https://doi.org/10.1126/scitranslmed.aaf9246	journal	October 2016
Structural and Functional Analysis of the Cdk13/Cyclin K Complex Greifenberg, Ann Katrin; Hönig, Dana; Pilarova, Kveta Cell Reports, Vol. 14, Issue 2 https://doi.org/10.1016/j.celrep.2015.12.025	journal	January 2016
Genome-wide Profiling of Genetic Synthetic Lethality Identifies CDK12 as a Novel Determinant of PARP1/2 Inhibitor Sensitivity Bajrami, I.; Frankum, J. R.; Konde, A. Cancer Research, Vol. 74, Issue 1 https://doi.org/10.1158/0008-5472.CAN-13-2541	journal	November 2013
Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains Martin, Mathew P.; Olesen, Sanne H.; Georg, Gunda I. ACS Chemical Biology, Vol. 8, Issue 11 https://doi.org/10.1021/cb4003283	journal	September 2013
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