Potent and selective proteasome inhibitor (Ki=0.6 nM). Inhibits proliferation of a number of tumor cell lines (IC50=7 nM). Inhibits TNFα synthesis and FGF-induced angiogenesis. Clinically useful agent for treatment of multiple myeloma.3 Shows promise in the treatment of neurodegenerative diseases in which low-expressing proteins such as IKAP/hELP1 in familial dysautonomia are preserved.4 Reversible. Cell permeable.
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2) Williams et al. (2003), Differential effects of the proteasome inhibitor bortezomib on apoptosis and angiogenesis in human prostate tumor xenografts; Mol. Cancer Ther., 2 835
3) Richardson et al. (2003), Bortezomib (PS-341): a novel, first-in-class proteasome inhibitor for the treatment of multiple myeloma and other cancers; Cancer Control, 10 361
4) Herve and Ibrahim (2017), Proteasome inhibitors to alleviate aberrant IKBKAP mRNA splicing and low IKAP/hELP1 synthesis in familial dysautonomia; Neurobiol. Dis., 103 113