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Hemi-synthetic trilobine analogs for use as DNA methylation inhibitors



Patents status

EPT 15306556 and EP 153065552 filed 2/10/2015


Yoann Menon
Christophe Long
Ludovic Halby
EB Kaloum
François Sautel
Paola B. Arimondo

commercial status

Exclusive or non-exclusive licenses





Epigenetic modifications play an essential role in the establishment and regulation of differentiation programs that define when and where genes are expressed. Among these modifications, C5 methylation of deoxycytidines (dC) in the DNA was shown to play a key role in the epigenetic regulation in mammals. The C5 DNA methyltransferases, DNMT, are responsible for DNA methylation Alterations of DNA methylation patterns lead to various diseases such as cancer and neurological diseases. Cancerous cells present aberrant DNA methylation, in particular a specific hypermethylation of tumour suppressor genes is observed inducing their silencing. Restoring their expression by specific inhibition of DNA methylation represents an attractive therapeutic strategy. In addition it has been shown that demethylating agents prime cancer cells towards immunotherapy and sensitize them towards chemotherapy.


Bisbenzylisoquinoline alkaloids and hemisynthetic derivatives developed in this invention can be used as DNMT inhibitors.


The compounds
Ø  inhibit the DNMT3A in the micromolar level (0.6µM)
Ø  demethylate gene promoters and induce gene expression in cancer cells
Ø  induce chromatin opening
Ø  reduce certain tumor phenotype of cancer cells


The compounds are able to inhibit DNA methylation in enzymatic assays, and to demethylate and reactivate genes when used at low doses for prolonged treatments.


The main application is as drugs for cancer treatment, mainly in combination with other epigenetic drugs or chemotherapy or immune-therapy

For further information, please contact us (Ref 09443-01 / 09443-02)

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