A Gold(III) Porphyrin Complex with Antitumor Properties Targets the Wnt/β-catenin Pathway

Kim Hei-Man Chow, Raymond Wai-Yin Sun, Janice B.B. Lam, Carrie Ka-Lei Li, Aimin Xu, Dik-Lung Ma, Ruben Abagyan, Yu Wang*, Chi-Ming Che*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

89 Citations (Scopus)

Abstract

Gold(III) complexes have shown promise as antitumor agents, but their clinical usefulness has been limited by their poor stability under physiological conditions. A novel gold(III) porphyrin complex [5-hydroxyphenyl-10,15,20-triphenylporphyrinato gold(III) chloride (gold-2a)] with improved aqueous stability showed 100-fold to 3,000-fold higher cytotoxicity than platinum-based cisplatin and IC50 values in the nanomolar range in a panel of human breast cancer cell lines. Intraductal injections of gold-2a significantly suppressed mammary tumor growth in nude mice. These effects are attributed, in part, to attenuation of Wnt/β-catenin signaling through inhibition of class I histone deacetylase (HDAC) activity. These data, in combination with computer modeling, suggest that gold-2a may represent a promising class of anticancer HDAC inhibitor preferentially targeting tumor cells with aberrant Wnt/β-catenin signaling.
Original languageEnglish
Pages (from-to)329–337
Number of pages9
JournalCancer Research
Volume70
Issue number1
DOIs
Publication statusPublished - 1 Jan 2010

Scopus Subject Areas

  • Oncology
  • Cancer Research

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