Anti-inflammatory Effect of a Cell-Penetrating Peptide Targeting the Nrf2/Keap1 Interaction | Zendy

Richard Steel | Zendy; Jonathan Cowan | Zendy; Estelle Payerne | Zendy; Maria A. O’Connell | Zendy; Mark Searcey | Zendy

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Anti-inflammatory Effect of a Cell-Penetrating Peptide Targeting the Nrf2/Keap1 Interaction

Author(s) -

Richard Steel,

Jonathan Cowan,

Estelle Payerne,

Maria A. O’Connell,

Mark Searcey

Publication year - 2012

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml300041g

Subject(s) - peptide , keap1 , inflammation , heme , tumor necrosis factor alpha , chemistry , regulator , microbiology and biotechnology , cytokine , negative regulator , signal transduction , cancer research , biology , biochemistry , gene , immunology , enzyme , transcription factor

Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is increasingly recognized as a central regulator of multiple signaling pathways in inflammation and cancer, and the ability to use chemical biological tools to investigate its biological effects is very attractive. A peptide comprising a TAT-conjugated Nrf2 sequence is shown to activate Nrf2 and its downstream target gene heme-oxygenase-1 (HO-1) in a dose-dependent manner in intact human THP-1 monocytes. Levels of Nrf2 protein peak after 3 h, whereas HO-1 mRNA and protein peak after 6 and 12 h, respectively. The peptide is also shown to inhibit the production of the pro-inflammatory cytokine TNF. The TAT-14mer constitutes a useful chemical biology tool with potential therapeutic applications.

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