The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents

@article{Lu2011TheTM,
  title={The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents},
  author={Wenjie Lu and Cong Xu and Zifan Pei and Abdelrahman S Mayhoub and Mark Cushman and David A. Flockhart},
  journal={Breast Cancer Research and Treatment},
  year={2011},
  volume={133},
  pages={99-109}
}
To improve the treatment of breast cancer, there has been a need for alternative aromatase inhibitors (AIs) that bring about adequate aromatase inhibition, while limiting side effects. Since two tamoxifen metabolites have been documented as AIs, we tested a wide range of tamoxifen metabolites on aromatase in order to better understand structural interactions with aromatase and constructed structure–function relationships as a first step toward the development of novel inhibitors. The ability of… CONTINUE READING