【摘 要】
：
The 3, 2-bisindole indirubin is a minor component of natural indigo, a 2, 2-bisindole representing a dye of worldwide use since ancient times.Specific indirubins are highly potent inhibitors of cyclin
【机 构】
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Department of Chemistry Division of Food Chemistry and Toxicology University of Kaiserslautern Germa
【出 处】
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BIT Life Sciences 1st Annual World Cancer Congess-2008(2008中
论文部分内容阅读
The 3, 2-bisindole indirubin is a minor component of natural indigo, a 2, 2-bisindole representing a dye of worldwide use since ancient times.Specific indirubins are highly potent inhibitors of cyclin dependent kinases (CDKs) that compete with ATP at the enzymes ATP binding site.In addition, indirubins have been shown to act as efficient inhibitors of further serine/threonine kinases, such as GSK-3β, as well as receptor/non-receptor tyrosine kinases, including VEGFR-2 (KDR) and c-Src.The respective potency of inhibition depends on chemical nature and position of substituents.In tumor cells, these compounds were found to induce dose dependent cell cycle arrest in G 1 and/or G2/M, leading to apoptosis with IC50 values for inhibition of tumor cell proliferation in the low micromolar to submicromolar range.
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