Identification of HSP60 as a Primary Target of o-Carboranylphenoxyacetanilide, an HIF-1α Inhibitor

被引：84

作者：

Ban, Hyun Seung ^{[1
]}

Shimizu, Kazuki ^{[1
]}

Minegishi, Hidemitsu ^{[1
]}

Nakamura, Hiroyuki ^{[1
]}

机构：

[1] Gakushuin Univ, Fac Sci, Dept Chem, Tokyo 1718588, Japan

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2010年 / 132卷 / 34期

关键词：

HYPOXIA-INDUCIBLE FACTOR-1-ALPHA; TUMOR-SUPPRESSOR PROTEIN; HIF-ALPHA; PATHWAY; UBIQUITYLATION; HYDROXYLATION; DEGRADATION; DERIVATIVES; COMPLEX; BIOLOGY;

D O I：

10.1021/ja104739t

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

We succeeded in the design and synthesis of multifunctional chemical probes of the HIF-1 alpha inhibitor carboranylphenoxyacetanilide (1) that combine photoaffinity labeling and click reaction to identify the target protein. HSP60 was identified as a primary target protein of 1 using the chemical probes 2 and 3. Furthermore, HSP60 inhibitor 4 suppressed hypoxia-induced HIF activation, indicating that HSP60 affects HIF-1 alpha accumulation directly or indirectly.

引用

页码：11870 / 11871

页数：2

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