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

• El‑Far Ali Hafez Ali MohammedTsuchiya Hiroshi Yamamoto Hazem M.E. Shaheen Yasser S. El‑Sayed Shuhei Kawano Sei‑Ichi Tanuma Yasuhiko Yamamoto

• Munesue Seiichi

• Harashima Ai

• Satoh Akira

• Shindo Mika

• Nakajima Shingo

• Inada Mana

• Tanaka Mariko

• Takeuchi Akihiko

• Tsuchiya Hiroyuki

• Yamamoto Hiroshi

• Shaheen Hazem M.E.

• El‑Sayed Yasser S.

• Kawano Shuhei

• Tanuma Sei‑Ichi

• Yamamoto Yasuhiko

• 棟居 聖一

• 原島 愛

• 武内　 章彦

• 土屋 弘行

• 山本 靖彦

抄録

金沢大学医薬保健研究域医学系

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.

Embargo Period 6 months

収録刊行物

• Oncology Letters

  Oncology Letters 15 (4), 4627-4634, 2018-04

  Spandidos Publications

キーワード

• Cancer malignancy
• Fibrosarcoma cells
• Papaverine
• Receptor for advanced glycation end-products

詳細情報

• CRID: 1390853650129117568
• NII論文ID: 120006605140
• DOI: 10.24517/00053847
• ISSN: 17921074
• Web Site: http://hdl.handle.net/2297/00053847
• 本文言語コード: en
• データソース種別:
  • JaLC
  • IRDB
  • CiNii Articles