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

Conclusion: We identified VPC-16230 as an ERα AF2 specific inhibitor that demonstrated promising anti-proliferative effect in breast cancer cell lines including TamR cells. VPC-16230 reduced the expression of ERα-inducible genes including CDC2, which is involved in cell division. We anticipate that the application of ERα AF2 inhibitors will provide a novel approach that can act as complementary therapeutics to treat ERα-positive tamoxifen-resistant and metastatic breast cancers.

http://breast-cancer-research.com/content/17/1/27

Source: Breast Cancer Research - February 25, 2015 Category: Cancer & Oncology Authors: Kriti SinghRavi MunugantiEric LeblancYu LinEuphemia LeungNada LallousMiriam ButlerArtem CherkasovPaul Rennie Source Type: research