Discovery and resistance mechanism of a selective CDK12 degrader

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders

(2020) Meng Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

CDK11 is required for transcription of replication-dependent histone genes

(2020) Pavla Gajdušková et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

CDK13 cooperates with CDK12 to control global RNA polymerase II processivity

(2020) Zheng Fan et al.   Science Advances

A dynamic view of the proteomic landscape during differentiation of ReNcell VM cells, an immortalized human neural progenitor line

(2019) Yuyu Song et al.   Scientific Data

Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

(2019) Yonghui Sun et al.   LEUKEMIA

CDK12 phosphorylates 4E-BP1 to enable mTORC1-dependent translation and mitotic genome stability

(2019) Seung H. Choi et al.   GENES & DEVELOPMENT

Overcoming BET inhibitor resistance in malignant peripheral nerve sheath tumors

(2019) Lu Q. Le et al.   CLINICAL CANCER RESEARCH

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

(2019) Baishan Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes

(2019) Lu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

CDK12 controls G1/S progression by regulating RNAPII processivity at core DNA replication genes

(2019) Anil Paul Chirackal Manavalan et al.   EMBO REPORTS

CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation

(2019) Malgorzata Krajewska et al.   Nature Communications

Ex vivo screen identifies CDK12 as a metastatic vulnerability in osteosarcoma

(2019) Ian Bayles et al.   JOURNAL OF CLINICAL INVESTIGATION

Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer

(2019) Victor Quereda et al.   CANCER CELL

EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma

(2018) Amanda Balboni Iniguez et al.   CANCER CELL

Structure-Based Design of Selective Noncovalent CDK12 Inhibitors

(2018) Jeffrey W. Johannes et al.   ChemMedChem

CDK12: an emerging therapeutic target for cancer

(2018) Goldie Y L Lui et al.   JOURNAL OF CLINICAL PATHOLOGY

Discovery of 3-Benzyl-1-(trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors

(2018) Masahiro Ito et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer

(2018) Dennis Dobrovolsky et al.   BLOOD

CDK12 regulates DNA repair genes by suppressing intronic polyadenylation

(2018) Sara J. Dubbury et al.   NATURE

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

(2017) Calla M Olson et al.   Nature Chemical Biology

Quantitative mass spectrometry-based multiplexing compares the abundance of 5000 S. cerevisiae proteins across 10 carbon sources

(2016) Joao A. Paulo et al.   Journal of Proteomics

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

(2016) Tinghu Zhang et al.   Nature Chemical Biology

Growth rate inhibition metrics correct for confounders in measuring sensitivity to cancer drugs

(2016) Marc Hafner et al.   NATURE METHODS

Non-canonical functions of cell cycle cyclins and cyclin-dependent kinases

(2016) Per Hydbring et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Cdk12 Is A Gene-Selective RNA Polymerase II Kinase That Regulates a Subset of the Transcriptome, Including Nrf2 Target Genes

(2016) Xuan Li et al.   Scientific Reports

Structural and Functional Analysis of the Cdk13/Cyclin K Complex

(2016) Ann Katrin Greifenberg et al.   Cell Reports

Characterization of Human Cyclin-Dependent Kinase 12 (CDK12) and CDK13 Complexes in C-Terminal Domain Phosphorylation, Gene Transcription, and RNA Processing

(2015) Kaiwei Liang et al.   MOLECULAR AND CELLULAR BIOLOGY

MultiNotch MS3 Enables Accurate, Sensitive, and Multiplexed Detection of Differential Expression across Cancer Cell Line Proteomes

(2014) Graeme C. McAlister et al.   ANALYTICAL CHEMISTRY

3' end formation of pre-mRNA and phosphorylation of Ser2 on the RNA polymerase II CTD are reciprocally coupled in human cells

(2014) L. Davidson et al.   GENES & DEVELOPMENT

The structure and substrate specificity of human Cdk12/Cyclin K

(2014) Christian A. Bösken et al.   Nature Communications

The Cyclin K/Cdk12 complex maintains genomic stability via regulation of expression of DNA damage response genes

(2011) D. Blazek et al.   GENES & DEVELOPMENT

MS3 eliminates ratio distortion in isobaric multiplexed quantitative proteomics

(2011) Lily Ting et al.   NATURE METHODS

MultiBac: expanding the research toolbox for multiprotein complexes

(2011) Christoph Bieniossek et al.   TRENDS IN BIOCHEMICAL SCIENCES

CDK12 is a transcription elongation-associated CTD kinase, the metazoan ortholog of yeast Ctk1

(2010) B. Bartkowiak et al.   GENES & DEVELOPMENT

Genomic instability — an evolving hallmark of cancer

(2010) Simona Negrini et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY