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   Articles with "cdk9" as a keyword



Inhibition of CDK9 enhances AML cell death induced by combined venetoclax and azacitidine.

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recommendations! Published in 2025 at "Molecular oncology"

DOI: 10.1002/1878-0261.70124

Abstract: Relapsed/refractory (R/R) disease is a major hurdle to long-term survival of acute myeloid leukemia (AML) patients treated with intensive cytarabine (AraC)-based chemotherapy. R/R AML salvage treatment with venetoclax (VEN) + azacitidine (AZA) results in overall response rates… read more here.

Keywords: cdk9; aml cell; arac; cell death ... See more keywords

Transient induction of Cdk9 in the early stage of differentiation is critical for myogenesis

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recommendations! Published in 2019 at "Journal of Cellular Biochemistry"

DOI: 10.1002/jcb.29204

Abstract: Cdk9 is a serine‐threonine protein kinase that has been recognized as a regulator of cardiac differentiation. Recently, we have reported that transient induction of Cdk9 using noncoding RNA targeting Cdk9 sequences results in efficient cardiac… read more here.

Keywords: transient induction; induction cdk9; cdk9; differentiation ... See more keywords

Design of Tat-Activated Cdk9 Inhibitor

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recommendations! Published in 2018 at "International Journal of Peptide Research and Therapeutics"

DOI: 10.1007/s10989-018-9730-9

Abstract: Virus mutates quickly and develops drug resistance over time if targeted directly. A possible alternative for drug design is to target cellular proteins that the virus needs. To be viable, the drug ought to inhibit… read more here.

Keywords: cdk9 cyclin; cdk9; drug; tat ... See more keywords

Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer

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recommendations! Published in 2018 at "Cell"

DOI: 10.1016/j.cell.2018.09.051

Abstract: Cyclin-dependent kinase 9 (CDK9) promotes transcriptional elongation through RNAPII pause release. We now report that CDK9 is also essential for maintaining gene silencing at heterochromatic loci. Through a live cell drug screen with genetic confirmation,… read more here.

Keywords: reactivates epigenetically; cdk9; genes cancer; cancer ... See more keywords
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The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer

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recommendations! Published in 2021 at "Cell"

DOI: 10.1016/j.cell.2021.04.022

Abstract: Gene expression by RNA polymerase II (RNAPII) is tightly controlled by cyclin-dependent kinases (CDKs) at discrete checkpoints during the transcription cycle. The pausing checkpoint following transcription initiation is primarily controlled by CDK9. We discovered that… read more here.

Keywords: integrator cdk9; transcription; pp2a integrator; cdk9 ... See more keywords

Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.

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recommendations! Published in 2021 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2021.113244

Abstract: Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to… read more here.

Keywords: cdk9 inhibitors; cdk9; structure based; selective cdk9 ... See more keywords

Addressing Transcriptional Dysregulation in Cancer through CDK9 Inhibition

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recommendations! Published in 2023 at "Biochemistry"

DOI: 10.1021/acs.biochem.2c00609

Abstract: Undermining transcriptional addiction, the dependence of cancers on selected transcriptional programs, is critically important for addressing cancers with high unmet clinical need. Cyclin-dependent kinase 9 (CDK9) has long been considered an actionable therapeutic target for… read more here.

Keywords: cdk9; transcriptional dysregulation; addressing transcriptional; dysregulation cancer ... See more keywords

Discovery and Administration Optimization of Novel Selective CDK9 Inhibitor, 1-7a-B1, for Improved Pharmacokinetics and Antitumor Efficacy In Vivo.

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recommendations! Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.5c00472

Abstract: Cyclin-dependent kinase 9 (CDK9) is a member of the transcriptional CDK subfamily. In this work, a de novo design strategy was used to obtain a series of novel CDK9 inhibitors. A novel selective CDK9 inhibitor… read more here.

Keywords: cdk9; cdk9 inhibitor; pharmacokinetics antitumor; improved pharmacokinetics ... See more keywords

Novel biallelic CDK9 variants are associated with retinal dystrophy without CHARGE-like malformation syndrome.

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recommendations! Published in 2025 at "Journal of human genetics"

DOI: 10.1038/s10038-025-01395-1

Abstract: Cyclin-dependent kinase 9 (CDK9) phosphorylates the C-terminal domain of RNA polymerase II (RNAPII) to regulate transcription. Previously, we reported that an 8-year-old boy with the biallelic CDK9 variants p.A288T and p.R303C exhibited a CHARGE-like malformation… read more here.

Keywords: malformation syndrome; cdk9; retinal dystrophy; dystrophy ... See more keywords

Efficacy of CDK9 inhibition in therapy of post-myeloproliferative neoplasm (MPN) secondary (s) AML cells

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recommendations! Published in 2022 at "Blood Cancer Journal"

DOI: 10.1038/s41408-022-00618-4

Abstract: Dear Editor, Signaling downstream of the pathogenetic mutations in JAK2, MPL, or calreticulin, along with co-occurring mutations in chromatin modifiers or transcription factors, results in dysregulated transcriptome and proteome that is responsible for the transformation… read more here.

Keywords: mpn saml; bay 1143572; treatment; post ... See more keywords

Glucocorticoid-induced phosphorylation by CDK9 modulates the coactivator functions of transcriptional cofactor GRIP1 in macrophages

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recommendations! Published in 2017 at "Nature Communications"

DOI: 10.1038/s41467-017-01569-2

Abstract: The glucocorticoid (GC) receptor (GR) suppresses inflammation by activating anti-inflammatory and repressing pro-inflammatory genes. GR-interacting protein-1 (GRIP1) is a GR corepressor in macrophages, however, whether GRIP1 mediates GR-activated transcription, and what dictates its coactivator versus… read more here.

Keywords: anti inflammatory; cdk9; inflammatory genes; grip1 ... See more keywords