RGD-modified angiogenesis inhibitor HM-3 dose: dual function during cancer treatment

Bioconjug Chem. 2011 Jul 20;22(7):1386-93. doi: 10.1021/bc2000929. Epub 2011 Jun 24.

Abstract

In the present study, we have undertaken pharmacodynamic studies of HM-3 in vitro and in vivo. A dual function of HM-3 with various doses was observed. HM-3 at low dose revealed obvious anticancer activity. In contrast, HM-3 at high dose had a tendency to promote tumorigenesis and tumor metastasis. Microarray analysis demonstrated that HM-3 at high dose could up-regulate the transcription of AKT1 and MEK1, which resulted in the promotion of tumorigenesis and metastasis. Therefore, the dose of angiogenesis inhibitors plays a critical role in cancer treatment. In order to achieve the ideal effect of angiogenesis inhibitor drugs on cancer treatment, a ful exploration of administration dose, frequency, and period for this kind of drugs is highly desired.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / administration & dosage
  • Angiogenesis Inhibitors / chemistry*
  • Angiogenesis Inhibitors / pharmacology
  • Angiogenesis Inhibitors / therapeutic use*
  • Animals
  • Cell Line
  • Cell Movement / drug effects
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Mice, Nude
  • Mitogen-Activated Protein Kinase 1 / genetics
  • Mitogen-Activated Protein Kinase 3 / genetics
  • Neoplasms / blood supply*
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Oligopeptides / administration & dosage
  • Oligopeptides / chemistry*
  • Oligopeptides / pharmacology
  • Oligopeptides / therapeutic use*
  • Organ Culture Techniques
  • Peptides / administration & dosage
  • Peptides / chemistry
  • Peptides / pharmacology
  • Peptides / therapeutic use
  • Proto-Oncogene Proteins c-akt / genetics

Substances

  • Angiogenesis Inhibitors
  • Oligopeptides
  • Peptides
  • arginyl-glycyl-aspartic acid
  • Proto-Oncogene Proteins c-akt
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3