An in vitro Study: Inhibitory Effect of Carfilzomib on Human Serum Paraoxonase-1 (hPON1)

Hakan Soyut

Background and Objective: hPON1 is an HDL-related lactonase that can inhibit LDL. It is considered atheroprotective. hPON1 contributes to the antioxidant function of HDL. It is believed that a decrease in PON1 activity may promote atherosclerosis. This article was aimed to investigate the inhibitory effect of carfilzomib on hPON1. Materials and Methods: In this study, we detect the inhibition between hPON1 and carfilzomib used in the treatment of myeloma. Results: We determined that carfilzomib showed very strong inhibitory properties for human serum PON1, with an IC₅₀ value of 43.31 μM and a mean K_i value of 44.37 μM. We determined that carfilzomib showed competitive inhibition. Conclusion: The use of carfilzomib, which has a very strong inhibitory effect, in the treatment of multiple myeloma can be very harmful.

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