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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.