Mechanism of action of superactive vitamin D analogs through regulated receptor degradation.

@article{Jskelinen2000MechanismOA,
  title={Mechanism of action of superactive vitamin D analogs through regulated receptor degradation.},
  author={Tiina J{\"a}{\"a}skel{\"a}inen and Sanna Ryh{\"a}nen and Anitta Mahonen and Hector F DeLuca and Pekka H. M{\"a}enp{\"a}{\"a}},
  journal={Journal of cellular biochemistry},
  year={2000},
  volume={76 4},
  pages={548-58}
}
We and others have previously shown that selected vitamin D analogs potentiate the vitamin D receptor (VDR) mediated transcription much more efficiently than the natural hormone itself. Here we show that the transcriptionally active 20-epi analogs, namely KH 1060 and MC 1288, protect VDR against degradation more efficiently than calcitriol at 10(-10) M concentration (VDR t(1/2) > 48 h, 17 h, and 10 h, respectively). The conformationally epi-like analog EB 1089 did not significantly alter the… CONTINUE READING