Epoxomicin is a potent proteasome inhibitor, primarily inhibiting the activity of CTRL(chymotrypsin-like proteasome). The novel α-epoxy ketone moiety of Epoxomicin forms covalent bonds with residues in particular catalytic subunits of the enzyme, disabling activity. The trypsin-like and peptidyl-glutamyl peptide hydrolyzing behavior of the proteasome were both inhibited by Epoxomicin as well (at 100 and 1,000-fold slower rates, respectively). Bone formation is heavily regulated by the ubiquitin-proteasome pathway, and Epoxomicin was shown to increase both bone volume and bone formation rates in rodents. Another study demonstrates that exposure to Epoxomicin and other proteasome inhibitors leads to dopaminergic cell death, producing a model of Parkinson's disease in vivo. Epoxomicin is an inhibitor of 20S Proteasome.
1. Hanada, M., et al. 1992. J. Antibiot. 45: 1746-1752. PMID: 1468981
2. Meng, L., et al. 1999. Proc. Natl. Acad. Sci. U.S.A. 96: 10403-10408. PMID: 10468620
3. Schwarz, K., et al. 2000. J. Immunol. 164: 6147-6157. PMID: 10843664
4. Princiotta, M.F., et al. 2001. Proc. Natl. Acad. Sci. U.S.A. 98: 513-518. PMID: 11149939
5. Garrett, I.R., et al. 2003. J. Clin. Invest. 111: 1771-1782. PMID: 12782679
6. McNaught, K.S., et al. 2004. Ann. Neurol. 56: 149-162. PMID: 15236415
See how others have used Epoxomicin. Click on the entry to view the PubMed entry .
PMID: # 28667089
Molinski, SV. et al. 2017. Orkambi® and amplifier co-therapy improves function from a rare CFTR mutation in gene-edited cells and patient tissue. EMBO Mol Med.
PMID: # 25264277
Lupino, E. et al. 2014. Exposure of neuroblastoma cell lines to imatinib results in the upregulation of the CDK inhibitor p27(KIP1) as a consequence of c-Abl inhibition. Biochemical pharmacology. 92: 235-50.
PMID: # 24385906
Caffarelli, N. et al. 2013. Cyclin A degradation by primate cytomegalovirus protein pUL21a counters its innate restriction of virus replication. PLoS Pathog.. 9: e1003825.
PMID: # 23604491
Orre, M. et al. 2013. Reactive glia show increased immunoproteasome activity in Alzheimer's disease. Brain. 136: 1415-31.
PMID: # 24023882
Prasad, R. et al. 2013. Blocking Plasmodium falciparum development via dual inhibition of hemoglobin degradation and the ubiquitin proteasome system by MG132. PLoS ONE. 8: e73530.
PMID: # 22702336
Uyama, M. et al. 2012. Regulation of osteoblastic differentiation by the proteasome inhibitor bortezomib. Genes Cells. 17: 548-58.
PMID: # 18757370
Shi, W. et al. 2008. Disassembly of MDC1 foci is controlled by ubiquitin-proteasome-dependent degradation. J. Biol. Chem.. 283: 31608-31616.
PMID: # 16332688
Um, JW. et al. 2006. Parkin ubiquitinates and promotes the degradation of RanBP2. J. Biol. Chem.. 281: 3595-3603.
PMID: # 16687393
Chen, IY. et al. 2006. Histone H2A.z is essential for cardiac myocyte hypertrophy but opposed by silent information regulator 2alpha. J. Biol. Chem.. 281: 19369-19377.
PMID: # 15632159
Fioriti, L. et al. 2005. Cytosolic prion protein (PrP) is not toxic in N2a cells and primary neurons expressing pathogenic PrP mutations. J. Biol. Chem.. 280: 11320-11328.
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