Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.

@article{Umemiya1997RegulationOR,
  title={Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.},
  author={Hiroki Umemiya and Hiroshi Fukasawa and Michiko Ebisawa and Laurence Douziech Eyrolles and Emiko Kawachi and G. Eisenmann and Hinrich Gronemeyer and Yoshihiro Hashimoto and Koichi Shudo and Hiroyuki Kagechika},
  journal={Journal of medicinal chemistry},
  year={1997},
  volume={40 26},
  pages={
          4222-34
        }
}
In human HL-60 promyelocytic leukemia cells, diazepinylbenzoic acid derivatives can exhibit either antagonistic or synergistic effects on the differentiation-inducing activities of natural or synthetic retinoids, the activity depending largely on the nature of the substituents on the diazepine ring. Thus, a benzolog of the retinoid antagonist LE135 (6), 4-(13H-10,11,12,13-tetrahydro-10, 10,13,13,15-pentamethyldinaphtho[2,3-b][1,2-e]diazepin-7-yl) benzoic acid (LE540, 17), exhibits a 1 order of… CONTINUE READING
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