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钙调蛋白抑制剂对白血病细胞生长的抑制作用:吩噻嗪类药物和蜂毒素。

Inhibition of growth of leukemic cells by inhibitors of calmodulin: phenothiazines and melittin.

作者信息

Hait W N, Grais L, Benz C, Cadman E C

出版信息

Cancer Chemother Pharmacol. 1985;14(3):202-5. doi: 10.1007/BF00258116.

DOI:10.1007/BF00258116
PMID:3995682
Abstract

Calmodulin, a ubiquitous calcium-binding protein, has recently been shown to play an important role in cellular proliferation. The calmodulin inhibitors melittin, trifluoperazine, and chlorpromazine inhibited the growth and clonogenicity of human and murine leukemic cells, and their potency reflected their activity as inhibitors of calmodulin. Melittin, which is a far more potent inhibitor of calmodulin activity, was also a more potent inhibitor of cell growth and clonogenicity. The less active phenothiazine metabolite, chlorpromazine sulfoxide, had much less potent cytotoxic activity.

摘要

钙调蛋白是一种普遍存在的钙结合蛋白,最近研究表明它在细胞增殖中发挥重要作用。钙调蛋白抑制剂蜂毒素、三氟拉嗪和氯丙嗪可抑制人和鼠白血病细胞的生长及克隆形成能力,其效力反映了它们作为钙调蛋白抑制剂的活性。蜂毒素作为钙调蛋白活性的一种更有效的抑制剂,也是细胞生长和克隆形成能力的更有效抑制剂。活性较低的吩噻嗪代谢物氯丙嗪亚砜具有弱得多的细胞毒性活性。

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Inhibition of growth of leukemic cells by inhibitors of calmodulin: phenothiazines and melittin.钙调蛋白抑制剂对白血病细胞生长的抑制作用:吩噻嗪类药物和蜂毒素。
Cancer Chemother Pharmacol. 1985;14(3):202-5. doi: 10.1007/BF00258116.
2
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2
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FEBS Lett. 1981 Oct 12;133(1):99-102. doi: 10.1016/0014-5793(81)80480-2.
3
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