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Informal seminar - Paola Arimondo : Targeting DNA methylation in cancer cells with non-nucleoside inhibitors

When Jan 23, 2017
from 02:00 PM to 03:00 PM
Where Genetics Part II Room
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Dr Paola Arimondo from CNRS, Pierre Fabre Centre for Research & Development, Toulouse

''Targeting DNA methylation in cancer cells with non-nucleoside inhibitors'' 

DNA methylation is involved in the regulation of gene expression and plays an important role in normal developmental processes and disease. In particular, the epigenetic landscape is altered in cancers where abnormal hypermethylation leads to silencing of certain genes such as tumor suppressor genes. In mammals, DNA methyltransferases are the enzymes responsible for DNA methylation on the position 5 of cytidine in a CpG context. Few direct enzyme inhibitors are known and those have several drawbacks. In order to identify novel inhibitors of DNA methylation, we applied three chemical strategies: High-Throughput Screening of chemical libraries, rational drug design based on molecular modeling and the pharmacomodulation of known inhibitors. The optimized inhibitor demethylate gene promoters and reactivate tumor suppressor genes. The discovery and the biological activity of the compounds will be illustrated as the study of their mechanism of action in cancer cells.

Host: Michaela Frye

If anyone would like to meet with the speaker individually please email Caroline Newnham by Wednesday 18th January.