Organogold compounds were developed originally as analogues of platinum based cytotoxic drugs like cisplatin. Although their strong antiproliferative effect, such compounds failed to be advanced into clinical trails due to their severe toxicity issue. GC20, a novel bis-chelated gold(I) diphosphine compound has shown strong anticancer potential and low toxicity in cancer cells and animal models. Based on its structural characteristics and biological properties, we hypothesized that GC20 might specifically inhibit selenoprotein TrxR while it might also intercalate with DNA. Thus, GC20 has potential to be developed into a single anticancer agent possessing both cytotoxic and target specific activities. Here, we systematically investigated the molecular mechanism of GC20. We measured the inhibition activities of GC20 on the thiol (seleno)-containing-proteins (TrxR, hTrxRU498C, hGR and Trx), and the interaction with GSH, DTT and fish DNA. Our preliminary results support our hypothesis and lay the foundation for further structural optimization of the organogold compounds.

Anticancer mechanism of a bis-chelated gold diphosphine compound

239th National Meeting (2010)

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