Transient induction of Cdk9 in the early stage of differentiation is critical for myogenesis
Sign Up to like & getrecommendations! 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
Sign Up to like & getrecommendations! 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
Sign Up to like & getrecommendations! 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
The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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
Sign Up to like & getrecommendations! 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
Efficacy of CDK9 inhibition in therapy of post-myeloproliferative neoplasm (MPN) secondary (s) AML cells
Sign Up to like & getrecommendations! 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
Sign Up to like & getrecommendations! 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
Function-guided proximity mapping unveils electrophilic-metabolite sensing by proteins not present in their canonical locales
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2120687119
Abstract: Significance The cell is a hive of information flow in which metabolite signals and proteins translocate across subcompartments. Peering into this submicroscopic world is hugely challenging. Using a strategy termed Localis-rex, we identify subcellular locale-specific… read more here.
Keywords: function; cdk9; electrophilic metabolite; proximity mapping ... See more keywords
Targeting AraC-Resistant Acute Myeloid Leukemia by Dual Inhibition of CDK9 and Bcl-2: A Systematic Review and Meta-Analysis
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Healthcare Engineering"
DOI: 10.1155/2022/2842066
Abstract: Purpose This study aims to determine the influence of targeting araC-resistant acute myeloid leukemia by dual inhibition cyclin-dependent protein kinase (CDK9) and B-cell lymphoma-2 （Bcl-2). Method The c-Myc inhibitor 10058-F4 and the CDK9 inhibitor AZD4573… read more here.
Keywords: myeloid leukemia; resistant acute; cdk9; targeting arac ... See more keywords
Abstract 4295: AZ’5576, a selective CDK9 inhibitor, demonstratesin vitroandin vivoactivity in diverse preclinical models of non-Hodgkin lymphoma
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-4295
Abstract: Cyclin-dependent kinase 9 (Cdk9) is a serine/threonine kinase that regulates elongation of transcription through phosphorylation of RNA polymerase II at serine 2 (pSer2-RNAPII). Transient inhibition of Cdk9 results in modulation of genes with short-lived transcripts… read more here.
Keywords: inhibitor; hodgkin lymphoma; cdk9; non hodgkin ... See more keywords