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Efficacy of cyclin-dependent-kinase 9 inhibitors in a murine model of mixed lineage leukemia

ABSTRACT: MLLENL transformed primary cells were treated for 6h with 250nM flavopiridol, PC585 or DMSO as control. RNA was isolated and analyzed on Agilent SurePrint G3 Mouse GE 8x60K (Agilent Microarray Design ID 028005) arrays.

ORGANISM(S): Mus musculus

SUBMITTER: Robert Slany 

PROVIDER: E-MEXP-3978 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress

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Efficacy of cyclin-dependent-kinase 9 inhibitors in a murine model of mixed-lineage leukemia.

Garcia-Cuellar M-P MP   Füller E E   Mäthner E E   Breitinger C C   Hetzner K K   Zeitlmann L L   Borkhardt A A   Slany R K RK  

Leukemia 20140121 7

Mixed-lineage leukemia fusion proteins activate their target genes predominantly by stimulating transcriptional elongation. A core component necessary for this activity is cyclin-dependent kinase 9. Here we explored the effectiveness of small molecules targeting this enzyme as potential therapeutics. A screen of seven compounds with anti-CDK9 activity applied to a panel of leukemia cell lines identified flavopiridol and the experimental inhibitor PC585 as superior in efficacy with inhibitory con  ...[more]

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