Identification of HSP60 as a Primary Target of o-Carboranylphenoxyacetanilide, an HIF-1α Inhibitor
- 9 August 2010
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 132 (34) , 11870-11871
- https://doi.org/10.1021/ja104739t
Abstract
We succeeded in the design and synthesis of multifunctional chemical probes of the HIF-1α 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-1α accumulation directly or indirectly.Keywords
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