Toward a New Chemotherapy for Breast Cancer: Structural and Functional Mechanism of the Retinoid Receptors Addressed by a Novel Computer Approach
Annual rept. 1 May 1990-30 Apr 2000
SCRIPPS RESEARCH INST LA JOLLA CA
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The Retinoid Receptors have been recognized for many years as targets for breast cancer therapy both in estrogen receptor-positive and -negative cells. However, their clinical use is limited, so far, because of toxic side effects. A better understanding at the biochemical and structural level of the molecular mechanism of retinoid action could result in the development of molecules with improved potency and reduced toxicity. We have undertaken a variety of computer modeling strategies to analyze the structural determinants for receptor and isoform specificity and the structural mechanism of agonist activity. Our efforts have already resulted in the identification of novel RAR agonists presenting very original features and we initiated a collaboration with renowned chemists and biologists to build on our findings and develop lead molecules against breast cancer.
- Anatomy and Physiology
- Medicine and Medical Research