A matrix metalloproteinase 2 cleavable melittin/avidin conjugate specifically targets tumor cells in vitro and in vivo

  • Authors:
    • Lori Holle
    • Wendy Song
    • Eric Holle
    • Yanzhang Wei
    • Thomas Wagner
    • Xianzhong Yu
  • View Affiliations

  • Published online on: January 1, 2003     https://doi.org/10.3892/ijo.22.1.93
  • Pages: 93-98
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Abstract

Extracellular matrix breakdown as well as increased expression in cancer cells and tumor microvascular endothelial cells make matrix metalloproteinase 2 (MMP2) an attractive target for cancer treatment. By taking advantage of MMP2's properties, an MMP2 cleavable melittin/avidin conjugate was designed. Melittin alone is extremely toxic to cells and induces immediate cell lysis, but becomes inactive when coupled with avidin. The incorporation of the MMP2 target sequence into the peptide was used as a means for targeting tumor cells. In vitro, the melittin/avidin conjugate showed strong cytolytic activity against cancer cells with high MMP2 activity; DU 145 prostate cancer cells and SK-OV-3 ovarian cancer cells. The conjugate exhibited very little cytolytic activity against normal L-cells that displayed low MMP2 activity. These data demonstrate the MMP2 specificity of the melittin/avidin conjugate. In vivo, the size of tumors injected with the melittin/avidin conjugate was significantly smaller as compared to untreated tumors. Therefore, due to its tumor targeting capabilities as well as its cytolytic properties in vitro and in vivo, the melittin/avidin conjugate displays the potential for use in cancer therapy.

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January 2003
Volume 22 Issue 1

Print ISSN: 1019-6439
Online ISSN:1791-2423

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APA
Holle, L., Song, W., Holle, E., Wei, Y., Wagner, T., & Yu, X. (2003). A matrix metalloproteinase 2 cleavable melittin/avidin conjugate specifically targets tumor cells in vitro and in vivo. International Journal of Oncology, 22, 93-98. https://doi.org/10.3892/ijo.22.1.93
MLA
Holle, L., Song, W., Holle, E., Wei, Y., Wagner, T., Yu, X."A matrix metalloproteinase 2 cleavable melittin/avidin conjugate specifically targets tumor cells in vitro and in vivo". International Journal of Oncology 22.1 (2003): 93-98.
Chicago
Holle, L., Song, W., Holle, E., Wei, Y., Wagner, T., Yu, X."A matrix metalloproteinase 2 cleavable melittin/avidin conjugate specifically targets tumor cells in vitro and in vivo". International Journal of Oncology 22, no. 1 (2003): 93-98. https://doi.org/10.3892/ijo.22.1.93