Toward a New Chemotherapy for Breast Cancer: Structural and Functional Mechanism of the Retinoid Receptors Addressed by a Novel Computer Approach
Abstract
Retinoids are known to be potent inhibitors of the proliferation of breast cancer cells, and recent observations have showed that they could be efficient molecular tools for breast cancer therapy. Our purpose is to help understand and control the activity of retinoid receptors, in order to design a new generation of drugs, more selective and efficacious, for breast cancer prevention and treatment. From a model of the active form of the Retinoid X Receptor (RXR), we could derive the determinants for retinoid receptor selectivity. We were then able to predict the mode of interaction between the Retinoic Acid Receptor (RAR) or RXR and known ligands. We also modeled the interaction between RAR or RXR and NRlF3, a novel nuclear receptor coactivator. Eventually, we discovered three novel agonists and two novel antagonists of RAR, which could lead to new drugs against breast cancer.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 1999
- Accession Number
- ADB257136
Entities
People
- Ruben A. Abagyan
Organizations
- NYU Langone Health