Quantitative comparison of the inhibitory effects of GW5638 and tamoxifen on angiogenesis in the cornea pocket assay

Sheng Tong, Qing Chen, Si Qing Shan, Mark W. Dewhirst, Fan Yuan

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

Abstract

GW5638 is a novel tissue-selective estrogen receptor (ER) modulator. Structurally, it is a derivative of tamoxifen that is known for its inhibitory effects on angiogenesis in an ER-independent manner. Therefore, it is possible that GW5638 has the same effects as tamoxifen on angiogenesis. To test this hypothesis, we used the rat cornea pocket assay and developed a new method that could precisely determine the total projected area of microvessels induced by basic fibroblast growth factor (bFGF) in the cornea. Animals in the study were treated with corn oil (control group), tamoxifen, or GW5638. After treatment, we observed that both GW5638 and tamoxifen could inhibit angiogenesis in the cornea (P<0.05) and that the inhibitory effects were not mediated by blocking functions of estrogen. Meanwhile, GW5638 had minimal effects on the body weight of animals whereas tamoxifen significantly reduced the body weight. Based on these observations, we concluded that GW5638 was as effective as tamoxifen in antiangiogenic treatment but less toxic than tamoxifen.

Original languageEnglish
Pages (from-to)53-58
Number of pages6
JournalAngiogenesis
Volume9
Issue number2
DOIs
StatePublished - Jun 2006

Bibliographical note

Funding Information:
The authors would like to thank Dr. Donald P. McDonnell for scientific discussion. The work supported in part by a grant from the Department of Defense (BC980191).

Keywords

  • Angiogenesis
  • Cornea pocket assay
  • DPC974
  • Estrogen receptor-modulator
  • GW5638

ASJC Scopus subject areas

  • Physiology
  • Clinical Biochemistry
  • Cancer Research

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