Recently the rrna synthesis inhibitors cx 5461 and bmh 21 have shown therapeutic potential in different cancer models 10 13 17. Here the authors show that cx 5461 a small molecule in clinical trials as rna polymerase inhibitor has g4 stablization properties and can be repurposed to target dna repair defective cancers cells.
Inhibition Of Pol I Transcription Treats Murine And Human Aml By
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In alamar blue cell viability assays cx 5461 had an average ic50 against 20 varied cell lines from those of pancreas prostate colorectal lung breast ovary etc of 78nm.
Cx 5461 mechanism of action. Cx 5461 is a first in class small molecule g quadruplex g4 stabiliser being developed for the treatment of haematological malignancies and solid tumours. To establish the pharmacokinetic pk profile of cx 5461. To evaluate the mechanism of action of cx 5461 in haematologic cancers.
Cx 5461 is the first potent and selective inhibitor of rna pol i transcription. These drugs have distinct mechanisms of action of inhibiting rrna synthesis. Cx 5461 is a potent and orally bioavailable inhibitor of pol i mediated rrna synthesis with ic50 s of 142 nm in hct 116 113 nm in a375 and 54 nm in mia paca 2 cells and shows little or no effect on pol ii ic50 25 mm.
To observe patients for evidence of cx 5461 biological activity using pharmacodynamic pd assessments. Cx 5461 adisinsight either you have javascript disabled or your browser does not support javascript. To observe patients for preliminary antitumor activity of cx 5461.
The compounds mechanism of action studies based on chip assay showed that drug interfered with sl1 induced assembly of pic.
Inhibition Of Pol I Transcription Treats Murine And Human Aml By
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