An in vitro study: Inhibitory effect of carfilzomib on human serum paraoxonase-1 (hpon1)

Abstract

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 mu M and a mean K-i value of 44.37 mu M. 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.