A gold(III) porphyrin complex with antitumor properties targets the Wnt/beta-catenin pathway.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 19996284.
- Also identified by DOI 10.1158/0008-5472.CAN-09-3324.
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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/beta-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/beta-catenin signaling.
Medical subject headings
- Antineoplastic Agents
- Gold Compounds
- Mammary Neoplasms, Experimental
- Metalloporphyrins
- Signal Transduction