Grant ID DP150096
Awarded On November 19, 2014
Title ESR1 Coregulator binding site inhibitors (ECBIs) as novel therapeutics to target hormone therapy resistant metastatic breast cancer
Program Academic Research
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
Contracted Amount $1,992,460
Lay Summary

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...

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