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EFFECTS OF METHOPRENE, ITS METABOLITES, AND BREAKDOWN PRODUCTS ON RETINOID-ACTIVATED PATHWAYS IN TRANSFECTED CELL LINES
Citation:
Schoff, P. K. AND G T. Ankley. EFFECTS OF METHOPRENE, ITS METABOLITES, AND BREAKDOWN PRODUCTS ON RETINOID-ACTIVATED PATHWAYS IN TRANSFECTED CELL LINES. ENVIRONMENTAL TOXICOLOGY AND CHEMISTRY. SETAC Press, Pensacola, FL, 23(5):1305-1310, (2004).
Description:
Methoprene is a terpene-based insecticide designed to act as an agonist of insect juvenile hormone, which is essential for the transition from larval to adult forms in some metamorphic insects. Recent evidence suggests that a methoprene metabolite, methoprene acid, activates a vertebrate retinoid X-receptor (RXR), and may interfere with retinoic acid-regulated developmental processes. Methoprene, methoxy-methoprene acid, and two major breakdown products were tested for their ability to interfere with retinoid-regulated pathways using two transfected cell lines. In the first, CV-1 cells were transiently transfected with genes encoding RXRs and response elements attached to luciferase reporters. The second line was derived from retinoic acid-sensitivity F9 cells, stably transfected with retinoic acid receptor (RAR)/RXR response elements attached a lacZ reporter. These experiments confirmed that methoxy-methoprene acid acted as a ligand for RXR and was capable of activating transcription through RAR/RXR response elements...Methoprene was as effective as the retinol dehydrogenase inhibitor citral in blocking the retinol-induced transcription of RAR/RXR-regulated reporter genes, while methoxy-methoprene acid blocked transcription stimulated by retinaldehyde.