Apomine, a novel hypocholesterolemic agent, accelerates degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase and stimulates low density lipoprotein receptor activity.

@article{Roitelman2004ApomineAN,
  title={Apomine, a novel hypocholesterolemic agent, accelerates degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase and stimulates low density lipoprotein receptor activity.},
  author={Joseph Roitelman and Dani{\`e}le Masson and Rachel Avner and Corinne Ammon-Zufferey and Anne Perez and Yves Guyon-Gellin and Craig L. Bentzen and Eric J Niesor},
  journal={The Journal of biological chemistry},
  year={2004},
  volume={279 8},
  pages={6465-73}
}
Apomine, a novel 1,1-bisphosphonate ester, has been shown to lower plasma cholesterol concentration in several species. Here we show that Apomine reduced the levels of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGR), the rate-limiting enzyme in the mevalonate pathway, both in rat liver and in cultured cells. Apomine resembles sterols such as 25-hydroxycholesterol in its ability to potently accelerate the rate of HMGR degradation by the ubiquitin-proteasome pathway, a process that depends… CONTINUE READING
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Mechanism of Apomine Action 6473 by gest on Sptem er 14

  • S. A. Jones, L. B. Moore, +9 authors J. T. Moore
  • November 19,
  • 2000
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