Identification and biological activities of a new antiangiogenic small molecule that suppresses mitochondrial reactive oxygen species

Ki Hyun Kim, Ju Yeol Park, Hye Jin Jung, Ho Jeong Kwon

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Mitochondrial reactive oxygen species (ROS) are associated with multiple cellular functions such as cell proliferation, differentiation, and apoptosis. In particular, high levels of mitochondrial ROS in hypoxic cells regulate many angiogenesis-related diseases, including cancer and ischemic disorders. Here we report a new angiogenesis inhibitor, YCG063, which suppressed mitochondrial ROS generation in a phenotypic cell-based screening of a small molecule-focused library with an ArrayScan HCS reader. YCG063 suppressed mitochondrial ROS generation under a hypoxic condition in a dose-dependent manner, leading to the inhibition of in vitro angiogenic tube formation and chemoinvasion as well as in vivo angiogenesis of the chorioallantoic membrane (CAM) at non-toxic doses. In addition, YCG063 decreased the expression levels of HIF-1α and its target gene, VEGF. Collectively, a new antiangiogenic small molecule that suppresses mitochondrial ROS was identified. This new small molecule tool will provide a basis for a better understanding of angiogenesis driven under hypoxic conditions.

Original languageEnglish
Pages (from-to)541-545
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume404
Issue number1
DOIs
Publication statusPublished - 2011 Jan 7

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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