Triciferol 是一种具有 VDR 激动剂和 HDAC 拮抗剂联合作用的多配体。Triciferol 直接与 VDR结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。抗增殖和细胞毒性活性。
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities[1].
Triciferol (0-10000 nM; 0-72 hours) is significantly more efficacious in suppressing the proliferation of estrogen receptor-negative human MDA-MB231 breast cancer cells[1].Treatment of MCF-7 cells with Triciferol (100-1000 nM) induces ≈2.5-fold higher rates of cell death than equimolar amounts of 1,25D[1].
参考文献:
[1]. Tavera-Mendoza LE, et al. Incorporation of histone deacetylase inhibition into the structure of a nuclear receptor agonist. Proc Natl Acad Sci U S A. 2008;105(24):8250-8255.
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