Identification of HSP60 as a Primary Target of o-Carboranylphenoxyacetanilide, an HIF-1α Inhibitor
HS Ban, K Shimizu, H Minegishi… - Journal of the American …, 2010 - ACS Publications
HS Ban, K Shimizu, H Minegishi, H Nakamura
Journal of the American Chemical Society, 2010•ACS PublicationsWe 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.
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.
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.
ACS Publications