|Awarded On||November 19, 2014|
|Title||ESR1 Coregulator binding site inhibitors (ECBIs) as novel therapeutics to target hormone therapy resistant metastatic breast cancer|
|Award Mechanism||Bridging the Gap: Early Translational Research Awards|
|Institution/Organization||The University of Texas Health Science Center at San Antonio|
|Principal Investigator/Program Director||Ratna Vadlamudi|
|Cancer Sites||Breast, Endocrine|
Endocrine therapies for estrogen receptor (ESR1) positive breast cancer involve modulation of ESR1 signaling using either antiestrogens (AE) or aromatase inhibitors (AI). Despite initial positive response, most patients develop resistance to these drugs and tumors recur as metastases. Resistant tumors retain ESR1-expression, acquire mutations and exhibit alterations in the levels and functions of coregulators that contribute to estrogen independent ESR1-signaling. There is a critical need to develop novel therapeutics that target ligand independent interaction of coregulators with ESR1.
AEs/AIs are ineffectual in disrupting ESR1 protein-protein interactions that occur in therapy-resistant an...