Ethaselen: a novel organoselenium anticancer agent targeting thioredoxin reductase 1 reverses cisplatin resistance in drug-resistant K562 cells by inducing apoptosis

@article{Ye2017EthaselenAN,
  title={Ethaselen: a novel organoselenium anticancer agent targeting thioredoxin reductase 1 reverses cisplatin resistance in drug-resistant K562 cells by inducing apoptosis},
  author={Suo-fu Ye and Yong Yang and Lin Wu and Wei-wei Ma and Hui-Hui Zeng},
  journal={Journal of Zhejiang University-SCIENCE B},
  year={2017},
  volume={18},
  pages={373-382}
}
It has been reported that Ethaselen shows inhibitory effects on thioredoxin reductase (TrxR) activity and human tumor cell growth. In order to find an efficient way to reverse cisplatin resistance, we investigated the reversal effects of Ethaselen on cisplatin resistance in K562/cisplatin (CDDP) cells that were established by pulse-inducing human erythrocyte leukemic cell line K562, which are fivefold more resistant to cisplatin compared to K562 cells. The morphology and growth showed that the… 
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A thioredoxin reductase inhibitor ethaselen induces growth inhibition and apoptosis in gastric cancer
TLDR
It is confirmed that the TrxR-targeting ethaselen could be a novel and effective drug for gastric cancer treatment and established a drug testing and screening system using GC-derived organoids by recapitulating tumor microenvironment.
Elucidating Role of Reactive Oxygen Species (ROS) in Cisplatin Chemotherapy: A Focus on Molecular Pathways and Possible Therapeutic Strategies
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Considering the relationship between ROS and CP chemotherapy, and translating these findings to clinic can pave the way for effective treatment of cancer patients.
Selenium and tellurium in the development of novel small molecules and nanoparticles as cancer multidrug resistance reversal agents.
Expanding the armory for treating lymphoma: Targeting redox cellular status through thioredoxin reductase inhibition.
Phenylselanyl Group Incorporation for “Glutathione Peroxidase-Like” Activity Modulation
TLDR
A new group of Se-based antioxidants, structurally derived from the well-known group of GPx mimics—benzisoselenazol-3(2H)-ones are presented.
Modulating ROS to overcome multidrug resistance in cancer.
Organic selenium compounds as potential chemotherapeutic agents for improved cancer treatment
Extracellular Albumin Covalently Sequesters Selenocompounds and Determines Cytotoxicity
TLDR
The importance of extracellular albumin binding in determining SeCs cytotoxicity was established and the formation of macromolecular conjugates between SeCs and albumin was confirmed.
Small molecule selenium-containing compounds: Recent development and therapeutic applications.
A general covalent binding model between cytotoxic selenocompounds and albumin revealed by mass spectrometry and X-ray absorption spectroscopy
TLDR
It is shown that cytotoxic SeCs could spontaneously transform into selenol intermediates that immediately react with albumin thiols through Se-S bond and the heterogeneous albumin binding degree may predict the variability in cytotoxicity.
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TLDR
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