Selective inhibitors of nuclear export (SINE)--a novel class of anti-cancer agents.

Selective inhibitors of nuclear export (SINE)--a novel class of anti-cancer agents.
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DOI:
10.1186/s13045-014-0078-0
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发表时间:
2014-10-15
影响因子:
28.5
通讯作者:
Liu D
Liu D
中科院分区:
医学1区
文献类型:
--
作者:
Parikh K;Cang S;Sekhri A;Liu D

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蛋白质核质转运的失调在肿瘤发生中起重要作用。蛋白质的核输出依赖于转运蛋白的活性。输出蛋白属于核转运蛋白β超家族。Exportin-1(XPO 1),也称为染色体区域维持1(CRM 1),介导约220种蛋白质的转运。本文综述了一类新型抗肿瘤药物--选择性核输出抑制剂(SINE)的研究进展。KPT-330(selinexor)作为口服药物在实体瘤和血液恶性肿瘤的早期临床试验中显示出活性。本文的在线版本(doi:10.1186/s13045-014-0078-0)包含补充材料,可供授权用户使用。
Dysregulation of the nucleo-cytoplasmic transport of proteins plays an important role in carcinogenesis. The nuclear export of proteins depends on the activity of transport proteins, exportins. Exportins belong to the karyopherin β superfamily. Exportin-1 (XPO1), also known as chromosomal region maintenance 1 (CRM1), mediates transport of around 220 proteins. In this review, we summarized the development of a new class of antitumor drugs, collectively known as selective inhibitors of nuclear export (SINE). KPT-330 (selinexor) as an oral agent is showing activities in early clinical trials in both solid tumors and hematological malignancies. The online version of this article (doi:10.1186/s13045-014-0078-0) contains supplementary material, which is available to authorized users.
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