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AK-1, a SIRT2 Inhibitor, Destabilizes HIF-1α and Diminishes Its Transcriptional Activity During Hypoxia

AK-1, a SIRT2 Inhibitor, Destabilizes HIF-1α and Diminishes Its Transcriptional Activity During Hypoxia

So Dam Lee, Wootae Kim, Joo-Won Jeong, Jong-Wan Park, Ja-Eun Kim

Cancer Lett. 2016 Apr 1;373(1):138-145.

PMID: 26808575

Abstract:

Sirtuin family proteins are involved in the regulation of hypoxic responses which are primarily dependent on a hypoxia-inducible factor (HIF). However, few studies have examined the use of sirtuin inhibitors to regulate HIF. The present study examined the effect of a SIRT2-specific inhibitor, AK-1, on hypoxic responses. Under hypoxic conditions, AK-1 increased the ubiquitination of HIF-1α in a VHL-dependent manner, leading to the degradation of HIF-1α via a proteasomal pathway. Downregulation of HIF-1α expression reduced its transcriptional activity and, eventually, reduced the expression of BNIP3, one of HIF-1 target genes, in AK-1-treated cells. These data demonstrate that SIRT2 inhibition attenuates hypoxic responses, and that SIRT2 inhibitors may have potential as treatments for hypoxia-associated pathological conditions.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP330461648-A	AK-1		330461-64-8	Price

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