Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome
Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome
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DOI：
10.1021/ml400531d
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发表时间：
2014-04-01
影响因子：
4.2
通讯作者：
Lin, Gang
中科院分区：
文献类型：
--
作者：
Fan, Hao;Angelo, Nicholas G.;Lin, Gang
人免疫蛋白酶体LMP7（β 5）亚基超过组成型蛋白酶体的选择性抑制剂有望用于治疗自身免疫性和炎性疾病以及血液恶性肿瘤。在这里，我们报告说，oxathiazolones抑制免疫蛋白酶体β 5i高达4700倍的选择性超过组成型蛋白酶体，是细胞渗透性，并抑制细胞内的蛋白酶体。
Selective inhibitors for the human immunoproteasome LMP7 (beta 5i subunit over the constitutive proteasome hold promise for the treatment of autoimmune and inflammatory diseases and hematologic malignancies. Here we report that oxathiazolones inhibit the immunoproteasome beta 5i with up to 4700-fold selectivity over the constitutive proteasome, are cell permeable, and inhibit proteasomes inside cells.