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Bortezomib


Mechanism of action:

Bortezomib is a reversible proteasome inhibitor. Because tumor cells rely on the 26S proteasome system to clear misfolded or regulatory proteins in order to sustain rapid growth, bortezomib reversibly binds to the β5 subunit of the 26S proteasome, leading to accumulation of misfolded proteins, triggering endoplasmic reticulum (ER) stress, causing cell cycle arrest at the G₂/M phase, and activating apoptosis-related pathways.

Reference(s):

1. Voorhees PM et al. (2003). The proteasome as a target for cancer therapy. Clin Cancer Res. 


2. Adams J et al. (1999). Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 


3. Berkers CR et al. (2005). Activity probe for in vivo profiling of the specificity of proteasome inhibitor bortezomib. Nat Methods.

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