In vitro anticancer effects of a RAGE inhibitor discovered using a structure-based drug design system

  • Authors:
    • Ali Hafez Ali Mohammed El‑Far
    • Seiichi Munesue
    • Ai Harashima
    • Akira Sato
    • Mika Shindo
    • Shingo Nakajima
    • Mana Inada
    • Mariko Tanaka
    • Akihiko Takeuchi
    • Hiroyuki Tsuchiya
    • Hiroshi Yamamoto
    • Hazem M.E. Shaheen
    • Yasser S. El‑Sayed
    • Shuhei Kawano
    • Sei‑Ichi Tanuma
    • Yasuhiko Yamamoto
  • View Affiliations

  • Published online on: January 29, 2018     https://doi.org/10.3892/ol.2018.7902
  • Pages:4627-4634
Metrics: HTML 0 views | PDF 0 views     Cited By (CrossRef): 0 citations

Abstract

Receptor for advanced glycation end-products (RAGE) is a pattern recognition receptor implicated in the pathogenesis of certain types of cancer. In the present study, papaverine was identified as a RAGE inhibitor using the conversion to small molecules through optimized‑peptide strategy drug design system. Papaverine significantly inhibited RAGE‑dependent nuclear factor κ‑B activation driven by high mobility group box‑1, a RAGE ligand. Using RAGE‑ or dominant‑negative RAGE‑expressing HT1080 human fibrosarcoma cells, the present study revealed that papaverine suppressed RAGE‑dependent cell proliferation and migration dose‑dependently. Furthermore, papaverine significantly inhibited cell invasion. The results of the present study suggested that papaverine could inhibit RAGE, and provided novel insights into the field of RAGE biology, particularly anticancer therapies.

Related Articles

Journal Cover

April 2018
Volume 15 Issue 4

Print ISSN: 1792-1074
Online ISSN:1792-1082

Sign up for eToc alerts

Recommend to Library

Copy and paste a formatted citation
APA
El‑Far, A.H., Munesue, S., Harashima, A., Sato, A., Shindo, M., Nakajima, S. ... Yamamoto, Y. (2018). In vitro anticancer effects of a RAGE inhibitor discovered using a structure-based drug design system. Oncology Letters, 15, 4627-4634. https://doi.org/10.3892/ol.2018.7902
MLA
El‑Far, A. H., Munesue, S., Harashima, A., Sato, A., Shindo, M., Nakajima, S., Inada, M., Tanaka, M., Takeuchi, A., Tsuchiya, H., Yamamoto, H., Shaheen, H. M., El‑Sayed, Y. S., Kawano, S., Tanuma, S., Yamamoto, Y."In vitro anticancer effects of a RAGE inhibitor discovered using a structure-based drug design system". Oncology Letters 15.4 (2018): 4627-4634.
Chicago
El‑Far, A. H., Munesue, S., Harashima, A., Sato, A., Shindo, M., Nakajima, S., Inada, M., Tanaka, M., Takeuchi, A., Tsuchiya, H., Yamamoto, H., Shaheen, H. M., El‑Sayed, Y. S., Kawano, S., Tanuma, S., Yamamoto, Y."In vitro anticancer effects of a RAGE inhibitor discovered using a structure-based drug design system". Oncology Letters 15, no. 4 (2018): 4627-4634. https://doi.org/10.3892/ol.2018.7902