Novel heparan sulfate mimetic compounds as antitumor agents

Keisuke Ishida, Michal K. Wierzba, Takayuki Teruya, Siro Simizu, Hiroyuki Osada

Research output: Contribution to journalArticle

39 Citations (Scopus)


Heparan sulfate glycosaminoglycans (HSGAGs) are involved in tumor cell growth, adhesion, invasion, and migration, due to their interactions with various proteins. In this study, novel HSGAG-mimetic compounds (KI compounds) were designed and synthesized. As a result of cell-based assays, KI-105 was found to exert potent inhibitory activities against migration and invasion of human fibrosarcoma HT1080 cells. The present results indicate that a novel invasion/migration inhibitor, KI-105, can increase the adherence of HT1080 cells. It was conceivable that this cellular effect was caused by an increase in the amount of cell-surface HSGAGs and focal adhesions. Although further investigations are needed to decipher the molecular mechanism of KI-105, it is suggested that heparanase and Cdc42 are involved in its biological effects.

Original languageEnglish
Pages (from-to)367-377
Number of pages11
JournalChemistry and Biology
Issue number3
Publication statusPublished - 2004 Mar 1
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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