Different biological targets for resiniferatoxin and phorbol 12-myristate 13-acetate.
The phorbol-related diterpene ester resiniferatoxin is at least 100-fold more inflammatory for the mouse ear than is the potent tumor promoter phorbol 12-myristate 13-acetate but is nonpromoting. We report here that resiniferatoxin is 100- to 1000-fold less active than is phorbol 12-myristate 13-acetate in in vitro assays with both chicken and mouse fibroblasts. These results suggest that resiniferatoxin and phorbol 12-myristate 13-acetate have different primary target sites (receptors) and provide further evidence that the fibroblast target may be homologous to that involved in promotion.
D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002478:Cells, Cultured; D002642:Chick Embryo; D003847:Deoxyglucose / Q000378:metabolism; D004224:Diterpenes / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005353:Fibronectins / Q000378:metabolism*; D007249:Inflammation / Q000139:chemically induced; D051379:Mice; D010704:Phorbols / Q000494:pharmacology*; D010960:Plasminogen Activators / Q000378:metabolism; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology*
D004224:Diterpenes; D005353:Fibronectins; D010704:Phorbols; D003847:Deoxyglucose; C024353:resiniferatoxin; D010960:Plasminogen Activators; D013755:Tetradecanoylphorbol Acetate