Epoxomicin
Epoxomicin structure
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Common Name | Epoxomicin | ||
|---|---|---|---|---|
| CAS Number | 134381-21-8 | Molecular Weight | 554.719 | |
| Density | 1.1±0.1 g/cm3 | Boiling Point | 795.7±60.0 °C at 760 mmHg | |
| Molecular Formula | C28H50N4O7 | Melting Point | 107-109ºC | |
| MSDS | Chinese USA | Flash Point | 435.0±32.9 °C | |
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Intramitochondrial adenylyl cyclase controls the turnover of nuclear-encoded subunits and activity of mammalian complex I of the respiratory chain.
Biochim. Biophys. Acta 1853(1) , 183-91, (2015) In mammalian cells the nuclear-encoded subunits of complex I are imported into mitochondria, where they are assembled with mt-DNA encoded subunits in the complex, or exchanged with pre-existing copies in the complex. The present work shows that in fibroblast ... |
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Ataxia telangiectasia mutated (ATM) inhibition transforms human mammary gland epithelial cells.
J. Biol. Chem. 285 , 13092-106, (2010) Carriers of mutations in the cell cycle checkpoint protein kinase ataxia telangiectasia mutated (ATM), which represent 1-2% of the general population, have an increased risk of breast cancer. However, experimental evidence that ATM deficiency contributes to h... |
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The ubiquitin-proteasome system regulates the stability and activity of the glucose sensor glucokinase in pancreatic β-cells.
Biochem. J. 456(2) , 173-84, (2013) The ubiquitin-proteasome system is important to maintain pancreatic β-cell function. Inhibition of the proteasome significantly reduced glucose-induced insulin secretion. Key regulators of the stimulus/secretion cascade seem to be affected by protein misfoldi... |
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Inhibition of the ubiquitin-proteasome pathway does not protect against ventilator-induced accelerated proteolysis or atrophy in the diaphragm.
Anesthesiology 121(1) , 115-26, (2014) Mechanical ventilation (MV) is a life-saving intervention in patients with acute respiratory failure. However, prolonged MV results in ventilator-induced diaphragm dysfunction (VIDD), a condition characterized by both diaphragm fiber atrophy and contractile d... |
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Tumor necrosis factor-α-induced apoptosis of gastric cancer MKN28 cells: accelerated degradation of the inhibitor of apoptosis family members.
Arch. Biochem. Biophys. 566 , 43-8, (2015) The role of the inhibitor of apoptosis (IAP) family members in tumor necrosis factor-α (TNF-α)-induced apoptosis of human gastric cancer MKN28 cells was explored. TNF-α induced up-regulation of cIAP2, whereas cycloheximide (CHX) induced down-regulation of XIA... |
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The proteasome inhibitor epoxomicin has potent Plasmodium falciparum gametocytocidal activity.
Antimicrob. Agents Chemother. 53 , 4080-5, (2009) Malaria continues to be a major global health problem, but only a limited arsenal of effective drugs is available. None of the antimalarial compounds commonly used clinically kill mature gametocytes, which is the form of the parasite that is responsible for m... |
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The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses.
J. Immunol. 164 , 6147, (2000) The complete inhibition of proteasome activities interferes with the production of most MHC class I peptide ligands as well as with cellular proliferation and survival. In this study we have investigated how partial and selective inhibition of the chymotrypsi... |
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Role of SUMO in RNF4-mediated promyelocytic leukemia protein (PML) degradation: sumoylation of PML and phospho-switch control of its SUMO binding domain dissected in living cells.
J. Biol. Chem. 284 , 16595-608, (2009) Promyelocytic leukemia protein (PML) is a tumor suppressor acting as the organizer of subnuclear structures called PML nuclear bodies (NBs). Both covalent modification of PML by the small ubiquitin-like modifier (SUMO) and non-covalent binding of SUMO to the ... |
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Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity.
Proc. Natl. Acad. Sci. U. S. A. 96 , 10403, (1999) The proteasome regulates cellular processes as diverse as cell cycle progression and NF-kappaB activation. In this study, we show that the potent antitumor natural product epoxomicin specifically targets the proteasome. Utilizing biotinylated-epoxomicin as a ... |
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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 , 513, (2001) The proteasome is the primary protease used by cells for degrading proteins and generating peptide ligands for class I molecules of the major histocompatibility complex. Based on the properties of cells adapted to grow in the presence of the proteasome inhibi... |