Proteasome inhibitor
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Proteasome inhibitor
Proteasome inhibitors are drugs that block the action of proteasomes, cellular complexes that break down proteins, like the p53 protein. Proteasome inhibitors are being studied in the treatment of cancer, especially multiple myeloma.
Examples
- In 2003, bortezomib was the first proteasome inhibitor to be approved for use in the U.S.
- Disulfiram has been proposed as another proteasome inhibitor.[1][2][3]
- Epigallocatechin-3-gallate has also been proposed.[4]
- Salinosporamide A has started clinical trials for multiple myeloma.
- carfilzomib has started phase II trials for multiple myeloma.[5]
- ONX 0912, CEP-18770, and MLN9708 have also started clinical trials.[5]
References
- ^ Lövborg H, Oberg F, Rickardson L, Gullbo J, Nygren P, Larsson R (March 2006). "Inhibition of proteasome activity, nuclear factor-KappaB translocation and cell survival by the antialcoholism drug disulfiram". International Journal of Cancer 118 (6): 1577–80. doi:10.1002/ijc.21534. PMID 16206267.
- ^ Wickström M, Danielsson K, Rickardson L, et al. (January 2007). "Pharmacological profiling of disulfiram using human tumor cell lines and human tumor cells from patients". Biochemical Pharmacology 73 (1): 25–33. doi:10.1016/j.bcp.2006.08.016. PMID 17026967.
- ^ Cvek B, Dvorak Z (August 2008). "The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?". Drug Discovery Today 13 (15-16): 716–22. doi:10.1016/j.drudis.2008.05.003. PMID 18579431.
- ^ Osanai K, Landis-Piwowar KR, Dou QP, Chan TH (August 2007). "A para-amino substituent on the D-ring of green tea polyphenol epigallocatechin-3-gallate as a novel proteasome inhibitor and cancer cell apoptosis inducer". Bioorg. Med. Chem. 15 (15): 5076–82. doi:10.1016/j.bmc.2007.05.041. PMC 2963865. PMID 17544279. http://linkinghub.elsevier.com/retrieve/pii/S0968-0896(07)00456-7.
- ^ a b "Current Advances in Novel Proteasome Inhibitor–Based Approaches to the Treatment of Relapsed/Refractory Multiple Myeloma". 2011. http://www.cancernetwork.com/supplements/onc-nov-2011/content/article/10165/1983430.
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