Bioactive Estrogen Conjugates

One of the major questions regarding the estrogen function is the nature and location of target receptors. Localization of estrogen receptor to regions like the plasma membrane and cytoplasm may give rise to unique signaling. We have conjugated a number of estrogen receptor ligands through linkers to different types of scaffolds to try to direct the drug to certain locations in a cell and study the cellular response.

The work on this project is a combination of synthetic chemistry (to make the conjugates), biochemistry (to test the activity of the conjugates in vitro and in cellular assays) and optical imaging (to see where the conjugates are located). We also plan to move to other nuclear receptor targets such as androgen receptor (for prostate cancer) and progesterone receptor (for contraceptive and fertility studies)

fluorescent conjugate

polymer conjugate

nanoparticle conjugate