S-adenosylhomocysteine (AdoHcy)-dependent methyltransferase inhibitor DZNep overcomes breast cancer tamoxifen resistance via induction of NSD2 degradation …
Q Wang, J Zheng, JX Zou, J Xu, F Han, S Xiang… - Chemico-Biological …, 2020 - Elsevier
Endocrine therapies (eg tamoxifen and aromatase inhibitors) targeting estrogen action are
effective in decreasing mortality of breast cancer. However, their efficacy is limited by
intrinsic and acquired resistance. Our previous study demonstrated that overexpression of a
histone methyltransferase NSD2 drives tamoxifen resistance in breast cancer cells and that
NSD2 is a potential biomarker of tamoxifen resistant breast cancer. Here, we found that
DZNep, an indirect inhibitor of histone methyltransferases, potently induces the degradation …
effective in decreasing mortality of breast cancer. However, their efficacy is limited by
intrinsic and acquired resistance. Our previous study demonstrated that overexpression of a
histone methyltransferase NSD2 drives tamoxifen resistance in breast cancer cells and that
NSD2 is a potential biomarker of tamoxifen resistant breast cancer. Here, we found that
DZNep, an indirect inhibitor of histone methyltransferases, potently induces the degradation …