DNA methylation inhibitors in cancer: recent and future approaches

…, L Halby, I Dufau, A Erdmann, JM Gregoire, F Ausseil… - Biochimie, 2012 - Elsevier
This review presents the different human DNA methyltransferases (DNMTs), their biological
roles, their mechanisms of action and their role in cancer. The description of assays for …

[HTML][HTML] Multicellular tumor spheroid model to evaluate spatio-temporal dynamics effect of chemotherapeutics: application to the gemcitabine/CHK1 inhibitor …

…, C Frongia, F Sicard, L Dedieu, P Cordelier, F Ausseil… - BMC cancer, 2012 - Springer
Background The multicellular tumor spheroid (MCTS) is an in vitro model associating
malignant-cell microenvironment and 3D organization as currently observed in avascular tumors. …

Parthenolide inhibits tubulin carboxypeptidase activity

X Fonrose, F Ausseil, E Soleilhac, V Masson, B David… - Cancer research, 2007 - AACR
Microtubules are centrally involved in cell division, being the principal components of mitotic
spindle. Tubulin, the constituent of microtubules, can be cyclically modified on its α-subunit …

Bioactive flavonoids of Tanacetum parthenium revisited

…, B David, C Lavaud, V Cassabois, F Ausseil… - Phytochemistry, 2003 - Elsevier
Bio-guided fractionation of an extract from Tanacetum parthenium showing activity as mitotic
blocker allowed the isolation and identification of santin 3, jaceidin 2 and centaureidin 1. …

Alisiaquinones and Alisiaquinol, Dual Inhibitors of Plasmodium falciparum Enzyme Targets from a New Caledonian Deep Water Sponge

…, D Dorin, C Doerig, A Valentin, F Ausseil… - Journal of natural …, 2008 - ACS Publications
Four new meroterpenes, alisiaquinones A−C (1−3) and alisiaquinol (4), were isolated from
a New Caledonian deep water sponge. Their structures and relative stereochemistry were …

[HTML][HTML] New insights on the mechanism of quinoline-based DNA Methyltransferase inhibitors

…, MH David-Cordonnier, I Dufau, F Ausseil… - Journal of Biological …, 2015 - ASBMB
Among the epigenetic marks, DNA methylation is one of the most studied. It is highly
deregulated in numerous diseases, including cancer. Indeed, it has been shown that …

Design, Synthesis and Biological Evaluation of 4‐Amino‐N‐(4‐aminophenyl)benzamide Analogues of Quinoline‐Based SGI‐1027 as Inhibitors of DNA Methylation

…, F Ausseil, F Sautel, PB Arimondo, F Cantagrel - …, 2014 - Wiley Online Library
Quinoline derivative SGI‐1027 (N‐(4‐(2‐amino‐6‐methylpyrimidin‐4‐ylamino)phenyl)‐4‐(quinolin‐4‐ylamino)benzamide)
was first described in 2009 as a potent inhibitor of DNA …

Rational design of bisubstrate-type analogues as inhibitors of DNA methyltransferases in cancer cells

…, A Samson, L Lacroix, F Ausseil… - Journal of Medicinal …, 2017 - ACS Publications
Aberrant DNA hypermethylation of promoter of tumor suppressor genes is commonly observed
in cancer, and its inhibition by small molecules is promising for their reactivation. Here we …

[HTML][HTML] Identification of a novel quinoline-based DNA demethylating compound highly potent in cancer cells

…, G Stazi, R Mazzone, R Fioravanti, C Gros, F Ausseil… - Clinical …, 2019 - Springer
Background DNA methyltransferases (DNMTs) are epigenetic enzymes involved in embryonic
development, cell differentiation, epithelial to mesenchymal transition, and control of gene …

Physalin B, a novel inhibitor of the ubiquitin-proteasome pathway, triggers NOXA-associated apoptosis

…, A Samson, Y Aussagues, G Massiot, F Ausseil… - Biochemical …, 2008 - Elsevier
The ubiquitin-proteasome pathway plays a critical role in the degradation of proteins involved
in tumor growth and has therefore become a target for cancer therapy. In order to discover …