Auranofin is a proteasomal deubiquitinase inhibitor with inhibition of the proteasome-associated deubiquitinases (DUBs) UCHL5 and USP14 rather than 20S proteasome, which is required for Auranofin-induced cytotoxicity. It selectively inhibits tumor growth in vivo and induces cytotoxicity in cancer cells from acute myeloid leukemia patients and by blocking NF-κB activation, Auranofin can attenuats the cardiac hypertrophy.
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Deubiquitinases (DUBs) are proteases that cleave ubiquitin or ubiquitin-like proteins from ubiquitin pro-proteins or conjugates with target proteins and they are responsible for maintenance of protein homeostasis in cells. Increased proteasome activity has been reported in many different cancers, such as colon and prostate cancers and leukemia, than in non-cancer cells, suggesting that DUBs are becoming attractive targets of cancer therapy. Auranofin inhibits proteasome-associated DUBs UCHL5 and USP14 rather than the 20S proteasome which is required for Auranofin-induced cytotoxicity. Auranofin reduced the cell viability via caspase activation in a dose-dependent manner with the IC50 values of 0.43 (24 h) and 0.17 μM (48 h) in HepG2 cells and 1.5 (24 h) and 0.41 μM (48 h) in MCF-7 cells, respectively[3]. Rats subjected to left ventricular hypertrophy via abdominal aorta constriction (AAC) showed enhanced chamber diameters and left ventricular function and decreased ejection fraction and fractional shortening values after intraperitoneal injections of 3 mg/kg Auranofin daily for 8 weeks, compared with AAC rats. Also, Auranofin treatment decreased proteasome activity and inactivation of the NF-κB signaling pathway in cardiac tissue[4]. Auranofin also shows potent bactericidal activities against M. tuberculosis, Bacillus subtilis, Enterococcus faecalis, Enterococcus faecium and Staphylococcus aureus[5].
作用机制
Auranofin inhibits 26S proteasome-associated DUBs UCHL5 and USP14 by targeting 19S RP.
Extensive Stage Small Cell Lun... 展开 >>g Carcinoma
Lung Adenocarcinoma
Recurrent Non-Small Cell Lung Carcinoma
Recurrent Small Cell Lung Carcinoma
Squamous Cell Lung Carcinoma
Stage IIIA Non-Small Cell Lung Cancer
Stage IIIB Non-Small Cell Lung Cancer
Stage IV Non-Small Cell Lung Cancer 收起 <<
Phase 1
Phase 2
Recruiting
November 2018
United States, Arizona
... 展开 >>
Mayo Clinic in Arizona
Recruiting
Scottsdale, Arizona, United States, 85259
Contact: Clinical Trials Referral Office 855-776-0015
Principal Investigator: Helen J. Ross 收起 <<
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