Selective antiestrogen binding site (aebs) ligands in the diphenyl methane series

We can offer and produce selective AEBS lignads for research purpose only.rnThese compounds are potent inducers of breast cancer cell differentiation and death

Interest / Relevance: The compounds are derivatives of the antiestrogen tamoxifen with no affinity for other target of tamoxifen such as estrogen receptors, PKC, ACAT or calmoduline.

Keywords: AEBS , sterol , oxysterol , apoptosis , autophagy

Scientist's name: Marc POIROT
Sandrine SILVENTE-POIROT

Publications:

Poirot et al Bioorg Med Chem 20008(8):2007-16rnPayre et al Mol Cancer Ther 20087(12):3707-18rnde Medina et al Cell Death Differ 2009 16(10):1372-84

Detailed technology overview: These compounds include PBPE (used in our lab as tool to study the AEBS) and tesmilifene (DPPE) that was developped by YMbioscience up to phase 3 clinical trials for anticancer applications. tesmilifene was stopped mainly because the clinical outcome in patient was not sufficient. The reason was the absence of understanding of its mechanism of action which led to a bad selection of patient and the expriration of the patent. Right now it is possible to reconsider the develpment of tesmilifene analogues based on the understanding of its molecular mechanism of action which has been solved recently by our team.

Reference:

RT00455