In silico discovery and validation of potent small-molecule inhibitors targeting the activation function 2 site of human oestrogen receptor α

Abstract

Current approaches to inhibit oestrogen receptor-alpha (ERα) are focused on targeting its hormone-binding pocket and have limitations. Thus, we propose that inhibitors that bind to a coactivator-binding pocket on ERα, called activation function 2 (AF2), might overcome some of these limitations. In silico virtual screening was used to identify small-molecule… (More)
DOI: 10.1186/s13058-015-0529-8

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@inproceedings{Singh2015InSD, title={In silico discovery and validation of potent small-molecule inhibitors targeting the activation function 2 site of human oestrogen receptor α}, author={Kriti Singh and Ravi Shashi Nayana Munuganti and Eric Leblanc and Yu Lun Lin and Euphemia Y Leung and Nada Lallous and M. H. Butler and Artem Cherkasov and Paul S. Rennie}, booktitle={Breast Cancer Research}, year={2015} }