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Table 1 Intracellular targets of bortezomib.

From: Preclinical evaluation of the proteasome inhibitor bortezomib in cancer therapy

Protein Function Effect of bortezomib References
IκBα Regulates the activity of the transcription factor, NF-κB Stabilization Hideshima et al [15], 2001
Russo et al [16], 2001
Sunwoo et al [17], 2001
Hideshima et al [18], 2002
Tan and Waldmann [19], 2002
Ma et al [20], 2003
JNK Phosphorylates and activates the transcription factor c-Jun Activation Hideshima et al [21], 2003
Chauhan et al [22], 2004
Yang et al [23], 2004
p21, p27 CDK inhibitors Stabilization Shah et al [24], 2001
Hideshima et al [15], 2001
Yang et al [23], 2004
p53 Transcription factor and Tumor suppressor Stabilization Williams and McConkey [25], 2003
Hideshima et al [21], 2003
Yang et al [23], 2004
Bid Proapoptotic protein Stabilization Breitschopf et al [26], 2000
Bax Proapoptotic protein Stabilization Li and Dou [27], 2000
Caveolin-1 Promotes cell migration Inhibition of activation Podar et al [28], 2004
gp130 Cytokine signaling receptor Downregulation Hideshima et al [29], 2003
DNA-PKcs DNA repair Cleavage Hideshima et al [21], 2003
ATM DNA repair Cleavage Hideshima et al [21], 2003
  1. IκBα = inhibitor κB-α; JNK = c-Jun-NH2 terminal kinase; CDK = cyclin-dependent kinase; DNA-PKcs = DNA protein kinase catalytic subunit; ATM = ataxia telangiectasia, mutated.