Resistance mechanism of bortezomib in multiple myeloma / 白血病·淋巴瘤

ABSTRACT

Bortezomib (BTZ), being the first proteasome inhibitor, has been applied widely in clinic. Through combining with targeting β5 subunit/chymotrypsin-like and inhibiting the activity of proteasome reversibly, BTZ manages to inhibit intracellular degradation of protein, thus inducing apoptosis of myeloma cells. Since 2000, when BTZ was approved by Food and Drug Administration (FDA) for treatment of multiple myeloma (MM), both response rates and long-term survival time of these patients have been improved significantly. However, most patients will inevitably end up with relapse or drug resistance due to its high heterogeneity. Thus, it is of great necessity to explore the mechanism as well as overcome BTZ resistance. This review aims to summarize the current researches available on mechanisms of BTZ resistance in MM.