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Human Cyclin-Dependent Kinase 12 (Cdk12), Kinase Domain; A Target Enabling Package

Research datakeyboard_double_arrow_right Dataset 17 Jun 2016Publisher:ZenodoFunded by:WT | A UK Hub to Catalyse Open...

Authors: Sarah E. Dixon-Clarke; Jonathan M. Elkins; S.-W. Grace Cheng; Tinghu Zhang; Nicholas Kwiatkowski; Calla M. Olson; Brian J. Abraham; +14 Authors

Human Cyclin-Dependent Kinase 12 (Cdk12), Kinase Domain; A Target Enabling Package

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Abstract

Cyclin-dependent kinase 12 (CDK12) phosphorylates RNA Pol II C-terminal domain (CTD) to promote transcriptional elongation of large DNA damage response genes. CDK12 is frequently mutated or amplified in cancer and its loss sensitises cells to DNA damage. Here we present 3 crystal structures of the human CDK12/CycK complex including apo, AMP-PNP and covalent inhibitor complexes. Kinase assays compare domain truncations and report the Km values for substrate. THZ531 is presented as a potent and selective inhibitor of CDK12 with nanomolar activity in leukemic cell lines.

This document represents version 3 of the TEP datasheet and includes all updates on the project as of April 2018. For more information about TEPs and the TEP Programme, please visit https://thesgc.org/tep.

Keywords

disease, structure discovery, infectious disease, malaria, chemical probe, chemical biology, structural genomics, metabolic diseases, drug target, drug discovery, neurological genetic disorders, oncology, target enabling package, cancer, neuropsychiatry, neuro, genetics, structure, orphan disease, protein, CDK12

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