Structure-based Discovery Of New Modulators Targeting Nuclear X Receptor Alpha For Cancer Therapy | 24155
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Retinoid X receptor-alpha (RXRα) is implicated in the regulation of many biological processes and also represents a unique
intracellular target for pharmacologic interventions. Efforts on discovery of small molecules targeting RXRα have been
primarily focused on the molecules that bind to its classical ligand-binding pocket (LBP). Using structure-based approach and
in collaboration with a multi-disciplinary team, we have identified novel RXRα modulators that use new binding mechanisms
to mediate the biological functions of RXRα. The new compounds can effectively suppress AKT activation and promotes
apoptosis of cancer cells in a RXRα-dependent manner by inhibiting the interaction between a truncated RXRα and the p85α
subunit of PI3K.
Ying Su, PhD, is computational chemist with over 15 years of experience on computer-aided drug design. She received her PhD from the University of California,
San Diego. After a postdoctoral appointment at the Scripps Research Institute, she worked for several local biotech companies. She joined the Sanford-Burnham
Medical Research Institute in 2005 to build and lead a HTS informatics and Cheminformticsgroup. She is co-author of over 40 peer-reviewed scientific publications.
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