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- | Journal: The HIV-1 Tat protein recruits a ubiquitin ligase to reorganize the 7SK snRNP for transcriptional activation. (Pubmed Central) - Apr 30, 2019
Finally, we demonstrate that UBE2O is critical for P-TEFb recruitment to the HIV-1 promoter. Together, the data support a unique model of elongation control where non-degradative ubiquitination of nuclear and cytoplasmic 7SK snRNP pools increases P-TEFb levels for transcriptional activation.
- | Nexavar (sorafenib) / Bayer, Amgen
Journal: Design and synthesis of novel imidazo[4,5-b]pyridine based compounds as potent anticancer agents with CDK9 inhibitory activity. (Pubmed Central) - Apr 24, 2019
Compounds showing significant anticancer activity revealed remarkable CDK9 inhibitory potential (IC = 0.63-1.32 μM) relative to sorafenib (IC = 0.76 μM). Moreover, a molecular docking study was performed to illustrate the binding mode of the most active compounds in the active site of CDK9 where it revealed superior binding affinity relative to the natural ligand (T3C).
- | Journal: Sirtuin 2-mediated deacetylation of cyclin-dependent kinase 9 promotes STAT1 signaling in type I interferon responses. (Pubmed Central) - Apr 18, 2019
These findings establish the existence of a previously unreported signaling pathway whose function is essential for the control of JAK-STAT signaling and the regulation of IFN responses. Our findings suggest that targeting sirtuin activities may offer an avenue in the development of therapies for managing immune-related diseases and cancer.
- | Journal: Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. (Pubmed Central) - Apr 17, 2019
Consistent with the degradation of the CDK9 protein, 11c selectively inhibits proliferation of CDK9-overexpressed cancer cells. Thus, our Wogonin-based PROTAC would be an efficient probe that induces the degradation of CDK9.
- | Venclexta (venetoclax) / Roche, AbbVie, alvocidib (DSP-2033) / Sumitomo Dainippon
Preclinical, Journal, IO Biomarker: Flavopiridol enhances ABT-199 sensitivity in unfavourable-risk multiple myeloma cells in vitro and in vivo. (Pubmed Central) - Apr 7, 2019
Thus, our Wogonin-based PROTAC would be an efficient probe that induces the degradation of CDK9. These findings argue that CDK9 inhibitors, for example, FP may increase the antimyeloma activity of ABT-199, including in unfavourable-risk MM minimally responsive to ABT-199 alone.British Journal of Cancer advance online publication, 14 December 2017; doi:10.1038/bjc.2017.432 www.bjcancer.com.
- | NMS-1116354 / Nerviano Medical Sciences
Journal: Repurposing of the CDK inhibitor PHA-767491 as a NRF2 inhibitor drug candidate for cancer therapy via redox modulation. (Pubmed Central) - Mar 29, 2019
We found that PHA-767491 treatment of multiple myeloma cells was associated with inhibition of nuclear translocation of NRF2, increased mitochondrial superoxide levels and inhibition of cell growth. Our findings suggest that PHA-767491 is a promising drug candidate for cancer therapy with NRF2 inhibitory potency contributing to its anti-cancer properties.
- | Journal: A stitch in time and CDK9. (Pubmed Central) - Mar 27, 2019
Our findings suggest that PHA-767491 is a promising drug candidate for cancer therapy with NRF2 inhibitory potency contributing to its anti-cancer properties. No abstract available
- | Journal: Long non-coding RNA EPIC1 promotes cholangiocarcinoma cell growth. (Pubmed Central) - Mar 27, 2019
RNA immunoprecipitation (RIP) results showed the direct interaction between Lnc-EPIC1 and Myc. Taken together, our results show that Lnc-EPIC1 promotes CCA cancer progression by targeting Myc.
- | Journal: Chromatin modifiers Mdm2 and RNF2 prevent RNA:DNA hybrids that impair DNA replication. (Pubmed Central) - Mar 23, 2019
Accordingly, RNase H overexpression or the inhibition of the transcription elongation kinase CDK9 each rescues DNA replication upon depletion of Mdm2 or RNF2. Taken together, our results suggest that chromatin modification by Mdm2 and PRC1 ensures smooth DNA replication through the avoidance of R-loop formation.
- | Journal: Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy. (Pubmed Central) - Mar 22, 2019
Cancer cell cycle analyses confirm that Cink4T blocks cells at both G/G and M phases as it should if it were to inhibit both Cdk4 and tubulin polymerization. Our results show, for the very first time, that virtual screening can be used to design novel inhibitors that can potently block two crucial phases of the cell division cycle.
- | atuveciclib (BAY 1143572) / Bayer
Journal: Antineoplastic effects of selective CDK9 inhibition with atuveciclib on cancer stem-like cells in triple-negative breast cancer. (Pubmed Central) - Jan 18, 2019
Finally, atuveciclib enhanced the antineoplastic effects of Cisplatin and promoted inhibitory effects on BCSLCs grown as mammospheres. Together, these findings suggest CDK9 as a potential therapeutic target in aggressive forms of CDK9-high TNBC.
- | azacitidine / Generic mfg.
Journal: RNA cytosine methylation and methyltransferases mediate chromatin organization and 5-azacytidine response and resistance in leukaemia. (Pubmed Central) - Dec 14, 2018
Both 5-AZA-resistant leukaemia cell lines and clinically 5-AZA-resistant myelodysplastic syndrome and acute myeloid leukaemia specimens have a significant increase in RNA:mC and NSUN1-/BRD4-associated active chromatin. This study reveals novel RNA:mC/RCMT-mediated chromatin structures that modulate 5-AZA response/resistance in leukaemia cells, and hence provides a new insight into treatment of leukaemia.