2. Academic Validation
  3. Identification of HSP60 as a primary target of o-carboranylphenoxyacetanilide, an HIF-1alpha inhibitor

Identification of HSP60 as a primary target of o-carboranylphenoxyacetanilide, an HIF-1alpha inhibitor

  • J Am Chem Soc. 2010 Sep 1;132(34):11870-1. doi: 10.1021/ja104739t.
Hyun Seung Ban 1,  Kazuki Shimizu,  Hidemitsu Minegishi,  Hiroyuki Nakamura
Affiliations

Affiliation

  • 1 Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Tokyo 171-8588, Japan.
PMID: 20695501 DOI: 10.1021/ja104739t
Abstract

We succeeded in the design and synthesis of multifunctional chemical probes of the HIF-1alpha 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-1alpha accumulation directly or indirectly.

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