Title : In silico screening for ERα down modulators identifies thioridazine as an anti-proliferative agent in primary, 4OH-tamoxifen-resistant and Y537S ERα-expressing breast cancer cells.

Pub. Date : 2018 Dec

PMID : 30182339






6 Functional Relationships(s)
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Protein Name
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1 In silico screening for ERalpha down modulators identifies thioridazine as an anti-proliferative agent in primary, 4OH-tamoxifen-resistant and Y537S ERalpha-expressing breast cancer cells. Thioridazine estrogen receptor 1 Homo sapiens
2 In silico screening for ERalpha down modulators identifies thioridazine as an anti-proliferative agent in primary, 4OH-tamoxifen-resistant and Y537S ERalpha-expressing breast cancer cells. Thioridazine estrogen receptor 1 Homo sapiens
3 RESULTS: We found that mitoxantrone and thioridazine induced ERalpha downmodulation and prevented MCF-7 BC cell proliferation. Thioridazine estrogen receptor 1 Homo sapiens
4 Thioridazine also reduced the ERalpha content and prevented cell proliferation in primary, Tam-resistant and genome-edited Y537S ERalpha expressing BC cells. Thioridazine estrogen receptor 1 Homo sapiens
5 Thioridazine also reduced the ERalpha content and prevented cell proliferation in primary, Tam-resistant and genome-edited Y537S ERalpha expressing BC cells. Thioridazine estrogen receptor 1 Homo sapiens
6 CONCLUSIONS: We suggest that modulation of the intracellular ERalpha concentration in BC cells can be exploited in in silico screens to identify anti-BC drugs and uncover a re-purposing opportunity for thioridazine in the treatment of primary and metastatic ET resistant BCs. Thioridazine estrogen receptor 1 Homo sapiens