This work highlights the importance of cancer cell intrinsic actions of estrogen receptor modulators in their therapeutic efficacy.
This study demonstrates that 27-hydroxycholesterol is a/the biochemical link between hypercholesterolemia/dyslipidemia and increased breast cancer risk and poor response to endocrine therapies. It resulted in several significant clinical trials to evaluate the impact of modulating 27-hydroxycholesterol on endocrine therapy in breast cancer.
Determined the mechanisms by which ERRα impacts breast cancer pathobiology and validated this receptor as a therapeutic target in cance
A discovery platform that exploits differential coregulator/NR interaction profiles to drive new drug discovery.
Demonstrated that receptor conformation and differential presentation of protein-protein interaction surfaces are the primary determinants of ER pharmacology and demonstrated the utility of disrupting protein-protein interaction surfaces as a therapeutic approach.
Study challenged the classical models of ER antagonist action and first to propose “functional allostery”.