Suberanilohydroxamic Acid as a Pharmacological Kruppel-Like Factor 2 Activator That Represses Vascular Inflammation and Atherosclerosis.

ABSTRACT:

Background

Kruppel-like factor 2 (KLF2) is an important zinc-finger transcription factor that maintains endothelial homeostasis by its anti-inflammatory, -thrombotic, -oxidative, and -proliferative effects in endothelial cells. In light of the potent vasoprotective effects of KLF2, modulating KLF2 expression or function could give rise to new therapeutic strategies to treat cardiovascular diseases.

Methods and results

High-throughput drug screening based on KLF2 promoter luciferase reporter assay was performed to screen KLF2 activators. Real-time PCR and western blot were used to detect gene and protein expression. Identified KLF2 activator was orally administered to ApoE^-/- mice to evaluate anti-atherosclerotic efficacy. By screening 2400 compounds in the Spectru

SUBMITTER: Xu Y 

PROVIDER: S-EPMC5779026 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature