Receptors as tools for understanding the toxicity of retinoids.
Retinoids are derivatives of vitamin A that have numerous biologic activities including induction of epithelial differentiation, pattern formation in embryos, and maintenance of spermatogenesis. Retinoids are used to treat various dermatologic maladies and specific forms of cancer but their use is limited by toxic liabilities: most notably teratogenesis. Retinoids interact with 2 families of receptors, the retinoic acid receptors (RARs) and retinoid X receptors (RXRs). The RARs and RXRs bind and transactivate distinct response elements of numerous genes. This multiplicity of receptors and gene products provides us with multiple targets for developing novel receptor-selective agonists. We are exploiting our knowledge of ligand receptor interactions to design better, more selective drugs and to understand the toxicity of retinoids and their metabolic products.
Levin
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Department of Toxicology and Pathology, Hoffmann-La Roche, Nutley, NJ, USA.
D000818:Animals; D006801:Humans; D018168:Receptors, Retinoic Acid / Q000502:physiology*; D047488:Retinoid X Receptors; D012176:Retinoids / Q000633:toxicity*; D014157:Transcription Factors / Q000502:physiology*
D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D012176:Retinoids; D014157:Transcription Factors