Interaction of cryptophycin 1 with tubulin and microtubules
Interaction of cryptophycin 1 with tubulin and microtubules
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DOI：
10.1016/0014-5793(95)01271-0
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发表时间：
1995-12-11
期刊：
影响因子：
3.5
通讯作者：
Himes, RH
中科院分区：
文献类型：
--
作者：
Kerksiek, K;Mejillano, MR;Himes, RH
隐藻素是从蓝藻中分离出来的新发现的抗有丝分裂药物，以往的研究表明微管是这些化合物的靶点，我们在体外研究了隐藻素1与微管蛋白和微管的相互作用，隐藻素1是一种有效的微管蛋白聚合抑制剂，使微管蛋白聚集。隐藻素1也抑制长春花碱与微管蛋白的结合，但不抑制秋水仙碱的结合，因此，隐藻素可能与微管蛋白中的长春花位点或与长春花位点重叠的位点结合。
The cryptophycins are newly discovered antimitotic agents isolated from the cyanobacterium Nostoc, Previous studies using cultured cells demonstrated that microtubules are the target of these compounds, We have studied the interaction of cryptophycin 1 with tubulin and microtubules in vitro, Cryptophycin 1 is an effective inhibitor of tubulin polymerization, causes tubulin to aggregate, and depolymerizes microtubules to linear polymers somewhat similar to the spiral-like structures produced by the Vinca alkaloids, Cryptophycin 1 also inhibits vinblastine binding to tubulin but not colchicine binding, Thus, it appears that the cryptophycins may bind to the Vinca site in tubulin or to a site that overlaps with the Vinca site.