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Updated: Jun 6, 2026

Transfer of Manipulated Tumor-associated Neutrophils into Tumor-Bearing Mice to Study their Angiogenic Potential In Vivo
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Transfer of Manipulated Tumor-associated Neutrophils into Tumor-Bearing Mice to Study their Angiogenic Potential In Vivo

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Effect of nitroxoline on angiogenesis and growth of human bladder cancer

Joong Sup Shim1, Yoshiyuki Matsui, Shridhar Bhat

  • 1Department of Pharmacology and Molecular Sciences, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA.

Journal of the National Cancer Institute
|November 20, 2010
PubMed
Abstract

Insights

Nitroxoline, an antibiotic, effectively inhibits MetAP2 activity and human umbilical vein endothelial cell proliferation. This compound demonstrates significant anti-tumor efficacy in preclinical models, showing promise as an antiangiogenic therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Angiogenesis is crucial for tumor growth and metastasis.
  • Inhibiting angiogenesis is a key strategy for novel anticancer drug development.
  • Type 2 methionine aminopeptidase (MetAP2) is a potential molecular target for antiangiogenic agents.

Purpose of the Study:

  • To identify MetAP2 inhibitors from existing clinical drugs.
  • To investigate the antiangiogenic and antitumor mechanisms of nitroxoline.
  • To evaluate nitroxoline's therapeutic potential as an antiangiogenic agent.

Main Methods:

  • High-throughput screening identified nitroxoline as a MetAP2 inhibitor.
  • In vitro assays assessed MetAP2 activity and HUVEC proliferation inhibition.
  • In vivo studies evaluated antiangiogenic effects and antitumor efficacy in breast and bladder cancer models.

Main Results:

  • Nitroxoline potently inhibited MetAP2 activity (IC50 = 54.8 nM) and HUVEC proliferation (IC50 = 1.9 μM).
  • Nitroxoline demonstrated antiangiogenic properties by inhibiting endothelial tube formation and reducing microvessel density.
  • Nitroxoline significantly reduced tumor volume in breast cancer xenografts and inhibited bladder cancer growth in vivo.

Conclusions:

  • Nitroxoline exhibits potent MetAP2 inhibitory activity.
  • Nitroxoline possesses significant antiangiogenic and antitumor effects.
  • Nitroxoline shows promise as a potential therapeutic antiangiogenic agent.

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