10.1080/14756366.2020.1844681
The research investigates the inhibitory effects of oxythiamine pyrophosphate (OTPP) and 3-deazathiamine pyrophosphate (DATPP) on the pyruvate dehydrogenase complex (PDHC) and their impact on HeLa cell growth. The study found that DATPP was a stronger competitive inhibitor of PDHC with a Ki value of 0.0026 mM compared to OTPP's Ki value of 0.025 mM. However, despite its superior inhibitory properties on PDHC, DATPP did not significantly affect HeLa cell growth or viability, whereas OTPP and oxythiamine (OT) showed a significant cytostatic effect. The researchers hypothesize that the differences in the cytostatic effects may be due to the physicochemical properties of the compounds and the difficulty in transporting DATPP across the cell membrane. The findings suggest that while DATPP is a potent inhibitor of PDHC, its effectiveness as a cytostatic agent may be limited by its cellular uptake and transport mechanisms.