Novel heparan sulfate mimetic compounds as antitumor agents

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

Research output: Contribution to journalArticlepeer-review

43 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
Externally publishedYes

ASJC Scopus subject areas

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


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