Epoxomicin Explained

Epoxomicin is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity.^[1] It was originally discovered in 1992.^[2] Injected, it can induce Parkinson's-like symptoms in rats.

Derivatives of epoxomicin include carfilzomib.

Further reading

• 1468981 . 45 . 11 . Epoxomicin, a new antitumor agent of microbial origin . November 1992 . J. Antibiot. . 1746–52 . 10.7164/antibiotics.45.1746. Hanada . M . Sugawara . K . Kaneta . K . Toda . S . Nishiyama . Y . Tomita . K . Yamamoto . H . Konishi . M . Oki . T . free .
• Meng . L. . 1999 . Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity . Proc. Natl. Acad. Sci. U.S.A. . 96 . 18. 10403–10408 . 10468620 . 10.1073/pnas.96.18.10403 . 17900. etal. free .
• Schwarz . K. . 2000 . The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses. J. Immunol. . 164 . 12. 6147–6157 . 10843664 . 2507740 . 10.4049/jimmunol.164.12.6147. etal.
• Princiotta . M.F. . 2001 . Cells adapted to the proteasome inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl sulfone require enzymatically active proteasomes for continued survival. Proc. Natl. Acad. Sci. U.S.A. . 98 . 2. 513–518 . 11149939 . 10.1073/pnas.021132398 . 14618. etal. free .
• Garrett . I.R. . 2003 . Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro. J. Clin. Invest. . 111 . 11. 1771–1782 . 12782679 . 10.1172/JCI16198 . 156102. etal.
• McNaught . K.S. . 2004 . Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease. Annals of Neurology . 56 . 1. 149–162 . 15236415 . 10.1002/ana.20186. 25314945 . etal.

Notes and References

1. 10.1073/pnas.96.18.10403 . PNAS . 1999 . 96 . Meng . 18 . L . 10403–10408 . Mohan . R . Kwok . BH . Elofsson . M . Sin . N . Crews . CM . Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity . 10468620 . 17900. free .
2. https://www.peptide.co.jp/en/new-product/314.html Epoxomicin