The mechanism of action and clinic trials of bortezomib in multiple myeloma

Bortezomib is a modified dipeptidyl boronic acid. Bortezomib is a reversible inhibitor of 26S proteasome, a large protein complex that degrades ubiquitinated proteins. The ubiquitinproteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within the cells. Inhibition of the proteasome pathway by bortezomib prevents the degradation of these intracellular proteins, affecting multiple signaling cascades within cells. This disruption of signaling cascades in cancer cells can lead to cell death and inhibit tumor growth.Multiple myeloma(MM) is a hematologic malignancy;despite the advent of high-dose chemotherapy with stem-cell transplantation, MM remains incurable.To compared with conventional chemotherapy, bortezomib has much anti-myeloma activity and less adverse effects.This review draws information both regarding the mechanism of proteasome inhibitor action and focuses on clinic trials from a range of studies in MM.