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Scientific article
English

Fulvene-5 potently inhibits NADPH oxidase 4 and blocks the growth of endothelial tumors in mice

Published inThe Journal of clinical investigation, vol. 119, no. 8, p. 2359-2365
Publication date2009
Abstract

Hemangiomas are the most common type of tumor in infants. As they are endothelial cell-derived neoplasias, their growth can be regulated by the autocrine-acting Tie2 ligand angiopoietin 2 (Ang2). Using an experimental model of human hemangiomas, in which polyoma middle T-transformed brain endothelial (bEnd) cells are grafted subcutaneously into nude mice, we compared hemangioma growth originating from bEnd cells derived from wild-type, Ang2+/-, and Ang2-/- mice. Surprisingly, Ang2-deficient bEnd cells formed endothelial tumors that grew rapidly and were devoid of the typical cavernous architecture of slow-growing Ang2-expressing hemangiomas, while Ang2+/- cells were greatly impaired in their in vivo growth. Gene array analysis identified a strong downregulation of NADPH oxidase 4 (Nox4) in Ang2+/- cells. Correspondingly, lentiviral silencing of Nox4 in an Ang2-sufficient bEnd cell line decreased Ang2 mRNA levels and greatly impaired hemangioma growth in vivo. Using a structure-based approach, we identified fulvenes as what we believe to be a novel class of Nox inhibitors. We therefore produced and began the initial characterization of fulvenes as potential Nox inhibitors, finding that fulvene-5 efficiently inhibited Nox activity in vitro and potently inhibited hemangioma growth in vivo. In conclusion, the present study establishes Nox4 as a critical regulator of hemangioma growth and identifies fulvenes as a potential class of candidate inhibitor to therapeutically interfere with Nox function.

Keywords
  • Angiopoietin-2/physiology
  • Animals
  • Cyclopentanes/ pharmacology
  • Endothelial Cells/metabolism
  • Enzyme Inhibitors/ pharmacology
  • Hemangioma/ drug therapy/pathology
  • Mice
  • NADPH Oxidase/ antagonists & inhibitors/genetics/physiology
  • Proteins/genetics
  • Vascular Endothelial Growth Factor A/antagonists & inhibitors
Citation (ISO format)
BHANDARKAR, S. S. et al. Fulvene-5 potently inhibits NADPH oxidase 4 and blocks the growth of endothelial tumors in mice. In: The Journal of clinical investigation, 2009, vol. 119, n° 8, p. 2359–2365. doi: 10.1172/JCI33877
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ISSN of the journal0021-9738
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