epoxomicin

a proteasome inihbitor, structure given in first source; from actinomycete strain Q996-17

Also Known As:

L-threoninamide, N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-((1S)-3-methyl-1-(((2R)-2-methyl-2-oxiranyl)carbonyl)butyl)-; N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-((1S)-3-methyl-1-(((2R)-2-methyl-2-oxiranyl)carbonyl)butyl)-L-threoninamide

Networked: 63 relevant articles (2 outcomes, 3 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Amino Acids, Peptides, and Proteins: 1
- Peptides: 82426
  - Oligopeptides: 519
    - epoxomicin: 63

Experts

1.	Asakura, Tadashi: 2 articles (05/2015 - 02/2004)
2.	Ohkawa, Kiyoshi: 2 articles (05/2015 - 02/2004)
3.	Kim, Kyung Bo: 2 articles (05/2013 - 09/2012)
4.	Prehn, J H M: 2 articles (10/2011 - 03/2007)
5.	Baker, Todd A: 2 articles (10/2010 - 12/2009)
6.	Gamelli, Richard L: 2 articles (10/2010 - 12/2009)
7.	Geng, Qing: 2 articles (10/2010 - 12/2009)
8.	Majetschak, Matthias: 2 articles (10/2010 - 12/2009)
9.	Picken, Maria M: 2 articles (10/2010 - 12/2009)
10.	Romero, Jacqueline: 2 articles (10/2010 - 12/2009)

Related Diseases

1.	Carcinoma (Carcinomatosis) 08/05/2004 - "The proteasome inhibitors, epoxomicin, lactacystin and carbobenzoxy-leucyl-leucyl-leucinal, stimulate the release of arachidonic acid from rat glial, human colon carcinoma, human breast carcinoma and the rat liver cells. " 05/15/2009 - "We quantitatively compared the efficacy of various proteasome inhibitors (MG132, lactacystin and epoxomicin) and IKK inhibitors (BAY 11-7082 and PS1145) to block NFkappaB activity induced by TNFalpha or TPA and to sensitize LNCaP prostate carcinoma cells to apoptosis. "
2.	Multiple Myeloma 05/01/2013 - "Epoxomicin also served as a scaffold for the generation of a synthetic tetrapeptide epoxyketone with improved activity, YU-101, which became the parent lead compound of carfilzomib (Kyprolis™), the recently approved therapeutic agent for multiple myeloma. "
3.	Melanoma (Melanoma, Malignant) 12/01/2017 - "In summary, this is the first study exploring molecular mechanisms of cell death induced by epoxomicin in melanoma. " 12/01/2017 - "Epoxomicin treatment also resulted in accumulation of Bcl-2 family members-proapoptotic Noxa and antiapoptotic Mcl-1, which were postulated as the targets for bortezomib in melanoma. " 07/01/2001 - "epoxomicin and N-benzyloxycarbonyl-Ile-Glu(O-tert-Bu)-Ala-leucinal (PSI) at a concentration of 1 microM did not affect cathepsin A activity in melanoma cell line lysates. " 12/01/2017 - "In this work, we analyze the cytotoxicity mechanisms of proteasome inhibitors (MG-132, epoxomicin, and lactacystin) in a specific form of melanoma which does not synthesize melanin-the amelanotic melanoma (Ab cells). " 06/28/2022 - "Our data show that epoxomicin-induced proteasome inhibition promoted both nicotinamide adenine dinucleotide phosphate oxidase and mitochondria-mediated oxidative stress and release of mitochondrial DNA to the cytosol, which resulted in potassium efflux-dependent absence in melanoma 2 (AIM2) inflammasome activation and subsequent interleukin-1β secretion in ARPE-19 cells. "
4.	Sepsis (Septicemia) 05/22/2014 - "Another goal was to assess the effects of administration of a specific proteasome inhibitor (epoxomicin, 0.5 mg/kg) on UPP response to sepsis. " 06/01/2009 - "The objective of this study was to determine if administration of proteasomal inhibitors (MG132, epoxomicin, bortezomib) can prevent sepsis-induced diaphragm weakness. "
5.	Malaria 12/01/2018 - "The proteasome of Plasmodium, the causative agent of malaria, has recently been validated as a target for anti-malarial drug development and therefore, in this study, we investigated the effect of epoxyketone (carfilzomib, ONX-0914 and epoxomicin) and boronic acid (bortezomib and ixazomib) proteasome inhibitors on the growth and survival of Babesia. "

Related Drugs and Biologics

1.	Proteasome Inhibitors
2.	benzyloxycarbonylleucyl-leucyl-leucine aldehyde
3.	carfilzomib
4.	lactacystin
5.	Tumor Necrosis Factor-alpha (Tumor Necrosis Factor)
6.	PS1145
7.	3- (4- methylphenylsulfonyl)- 2- propenenitrile
8.	Bortezomib (Velcade)
9.	Proteasome Endopeptidase Complex (Proteasome)
10.	Boronic Acids

Related Therapies and Procedures

1.	Induced Heart Arrest (Cardioplegia)
2.	Aftercare (After-Treatment)