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Auranofin is a synthetic gold(I) complex originally developed for the treatment of rheumatoid arthritis. Its structure features a gold atom coordinated with triethylphosphine and a thiolate ligand derived from a sugar (often referred to as a thiosugar).
Pathways:
1.Thioredoxin Reductase (TrxR) Inhibition.
- Most widely recognized for potently inhibiting TrxR.
2.Induction of Reactive Oxygen Species (ROS) and Oxidative Stress.
3.MMP depolarization, release of cytochrome c
4.Endoplasmic Reticulum (ER) Stress and Unfolded Protein Response (UPR)
5.Inhibition of Pro-survival Pathways (e.g., NF-κB Signaling)
-ic50 for cancer typically 1-3uM, normal cell 5-10uM or higher.
-Several studies animal testing antitumor efficacy have used doses in the region of 5–8 mg/kg via intraperitoneal injection or oral administration.
-Auranofin’s anticancer activity is often linked to its inhibition of thioredoxin reductase, leading to increased oxidative stress.