A new pharmacological agent (AKB-4924) stabilizes hypoxia inducible factor-1 (HIF-1) and increases skin innate defenses against bacterial infection

CYM Okumura, A Hollands, DN Tran, J Olson… - Journal of molecular …, 2012 - Springer
CYM Okumura, A Hollands, DN Tran, J Olson, S Dahesh, M von Köckritz-Blickwede…
Journal of molecular medicine, 2012Springer
Abstract Hypoxia inducible factor-1 (HIF-1) is a transcription factor that is a major regulator of
energy homeostasis and cellular adaptation to low oxygen stress. HIF-1 is also activated in
response to bacterial pathogens and supports the innate immune response of both
phagocytes and keratinocytes. In this work, we show that a new pharmacological compound
AKB-4924 increases HIF-1 levels and enhances the antibacterial activity of phagocytes and
keratinocytes against both methicillin-sensitive and methicillin-resistant strains of …
Abstract
Hypoxia inducible factor-1 (HIF-1) is a transcription factor that is a major regulator of energy homeostasis and cellular adaptation to low oxygen stress. HIF-1 is also activated in response to bacterial pathogens and supports the innate immune response of both phagocytes and keratinocytes. In this work, we show that a new pharmacological compound AKB-4924 increases HIF-1 levels and enhances the antibacterial activity of phagocytes and keratinocytes against both methicillin-sensitive and methicillin-resistant strains of Staphylococcus aureus in vitro. AKB-4924 is also effective in stimulating the killing capacity of keratinocytes against the important opportunistic skin pathogens Pseudomonas aeruginosa and Acinetobacter baumanii. The effect of AKB-4924 is mediated through the activity of host cells, as the compound exerts no direct antimicrobial activity. Administered locally as a single agent, AKB-4924 limits S. aureus proliferation and lesion formation in a mouse skin abscess model. This approach to pharmacologically boost the innate immune response via HIF-1 stabilization may serve as a useful adjunctive treatment for antibiotic-resistant bacterial infections.
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