Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20S proteasome.

Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20S proteasome.
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DOI:
10.1021/np300231f
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发表时间:
2012-05-25
影响因子:
5.1
通讯作者:
Tepe JJ
Tepe JJ
中科院分区:
生物学2区
文献类型:
--
作者:
Lansdell TA;Hewlett NM;Skoumbourdis AP;Fodor MD;Seiple IB;Su S;Baran PS;Feldman KS;Tepe JJ

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我们在此报道了oroidin衍生的生物碱帕劳'amine(1)、dibromophakellin(2)和dibromophakellstatin(3)抑制人20S蛋白酶体以及i20S免疫蛋白酶体催化核心的蛋白水解活性。发现帕劳'胺可防止细胞培养物中泛素化蛋白(包括IκBα)的降解,这可能表明这些药物显示其令人兴奋的细胞毒性和免疫抑制特性的潜在机制。
We report herein that the oroidin-derived alkaloids, palau’amine (1), dibromophakellin (2) and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the i20S immunoproteasome catalytic core. Palau’amine is found to prevent the degradation of ubiquitinylated proteins, including IκBα, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties.
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