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   Articles with "cdk12" as a keyword



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CDK12 inhibition enhances sensitivity of HER2+ breast cancers to HER2-tyrosine kinase inhibitor via suppressing PI3K/AKT.

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recommendations! Published in 2021 at "European journal of cancer"

DOI: 10.1016/j.ejca.2020.11.045

Abstract: BACKGROUND Alhtough anti-HER2 tyrosine kinase inhibitors (TKIs) have radically prolonged survival and improved prognosis in HER2-positive breast cancer patients, resistance to these therapies is a constant obstacle leading to TKIs treatment failure and tumour progression.… read more here.

Keywords: breast; anti her2; inhibition; cdk12 ... See more keywords

Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13

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recommendations! Published in 2022 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.2c00384

Abstract: Selective degradation of the cyclin-dependent kinases 12 and 13 (CDK12/13) presents a novel therapeutic opportunity for triple-negative breast cancer (TNBC), but there is still a lack of dual CDK12/13 degraders. Here, we report the discovery… read more here.

Keywords: cdk12; highly potent; cdk12 cdk13; selective dual ... See more keywords

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

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recommendations! Published in 2019 at "Nature Communications"

DOI: 10.1038/s41467-019-09703-y

Abstract: Cyclin-dependent kinase 12 (CDK12) modulates transcription elongation by phosphorylating the carboxy-terminal domain of RNA polymerase II and selectively affects the expression of genes involved in the DNA damage response (DDR) and mRNA processing. Yet, the… read more here.

Keywords: dna damage; polyadenylation; damage response; cdk12 ... See more keywords
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Discovery and resistance mechanism of a selective CDK12 degrader

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recommendations! Published in 2021 at "Nature Chemical Biology"

DOI: 10.1038/s41589-021-00765-y

Abstract: Cyclin-dependent kinase 12 (CDK12) is an emerging therapeutic target due to its role in regulating transcription of DNA-damage response (DDR) genes. However, development of selective small molecules targeting CDK12 has been challenging due to the… read more here.

Keywords: bsj 116; discovery resistance; mechanism; degrader ... See more keywords

CDK12 is a potential biomarker for diagnosis, prognosis and immunomodulation in pan-cancer

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recommendations! Published in 2024 at "Scientific Reports"

DOI: 10.1038/s41598-024-56831-7

Abstract: Cell cycle-dependent protein kinase 12 (CDK12) plays a key role in a variety of carcinogenesis processes and represents a promising therapeutic target for cancer treatment. However, to date, there have been no systematic studies addressing… read more here.

Keywords: cancer; diagnosis prognosis; cdk12 potential; cdk12 ... See more keywords

DNA2 protein destruction dictates DNA hyperexcision, cGAS–STING activation, and innate immune response in CDK12-deregulated cancers

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recommendations! Published in 2025 at "Proceedings of the National Academy of Sciences of the United States of America"

DOI: 10.1073/pnas.2413732122

Abstract: Significance The protein kinase gene CDK12 is frequently altered genetically in human cancers including prostate, ovarian, and breast cancer. Loss of CDK12 has been linked to enhanced anticancer immunity in prostate cancer. Here, we report… read more here.

Keywords: dna2 protein; cdk12; immune response; response cdk12 ... See more keywords

A patent and literature review of CDK12 inhibitors

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recommendations! Published in 2022 at "Expert Opinion on Therapeutic Patents"

DOI: 10.1080/13543776.2022.2126765

Abstract: ABSTRACT Introduction Cyclin-dependent kinase 12 (CDK12) belongs to the CDK family of serine/threonine protein kinases and is associated with cyclin K to exert its biological functions, including regulating gene transcription, mRNA processing, and translation. Increasing… read more here.

Keywords: cdk12; patent literature; literature review; cdk12 inhibitors ... See more keywords

Cdk12 Regulates Neurogenesis and Late‐Arising Neuronal Migration in the Developing Cerebral Cortex

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recommendations! Published in 2017 at "Cerebral Cortex"

DOI: 10.1093/cercor/bhw081

Abstract: Abstract DNA damage response (DDR) pathways are critical for ensuring that replication stress and various types of DNA lesion do not perturb production of neural cells during development. Cdk12 maintains genomic stability by regulating expression… read more here.

Keywords: cerebral cortex; mutant mice; late arising; migration ... See more keywords

#2061 Tubule-specific cyclin-dependent kinase 12 knockdown promotes fatty acid oxidation disorder by down-regulating PPARγ in chronic kidney disease

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recommendations! Published in 2025 at "Nephrology Dialysis Transplantation"

DOI: 10.1093/ndt/gfaf116.0402

Abstract: Chronic kidney disease (CKD) is a common kidney disease with high mortality and disability, which has caused serious health burden worldwide. Renal fibrosis plays a critical role in the progression of CKD to end-stage renal… read more here.

Keywords: ckd; disease; cdk12; renal tubular ... See more keywords

CDK12 Is Necessary to Promote Epidermal Differentiation Through Transcription Elongation.

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recommendations! Published in 2022 at "Stem cells"

DOI: 10.1093/stmcls/sxac002

Abstract: Proper differentiation of the epidermis is essential to prevent water loss and to protect the body from the outside environment. Perturbations in this process can lead to a variety of skin diseases that impacts 1… read more here.

Keywords: cdk12; epidermal differentiation; elongation; transcription elongation ... See more keywords

CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model

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recommendations! Published in 2020 at "Science Translational Medicine"

DOI: 10.1126/scitranslmed.aaz2415

Abstract: CDK12 inhibition reduces mutant transcripts and nuclear foci in DM1 cells and produces splicing correction and phenotypic benefit in a mouse model. Muscling in on myotonic dystrophy Myotonic dystrophy type 1 (DM1) is a genetic… read more here.

Keywords: dm1; nuclear foci; inhibition; myotonic dystrophy ... See more keywords