AI Article Synopsis
- Ebselen is an organo-selenium drug known for its various pharmacological effects, mainly by affecting redox systems through interactions with seleno enzymes like glutathione peroxidase and thioredoxin reductase.
- The drug also forms covalent bonds with thiol groups in various enzymes and has been explored in clinical trials for treating and preventing different health conditions.
- Researchers synthesized two coumarin-tagged probes that incorporate the ebselen component for further biological studies, differing by their spacer structure, and examined their interactions with cysteine proteases.
Article Abstract
The organo-seleniumdrug ebselen exhibits a wide range of pharmacological effects that are predominantly due to its interference with redox systems catalyzed by seleno enzymes, e.g., glutathione peroxidase and thioredoxin reductase. Moreover, ebselen can covalently interact with thiol groups of several enzymes. According to its pleiotropic mode of action, ebselen has been investigated in clinical trials for the prevention and treatment of different ailments. Fluorescence-labeled probes containing ebselen are expected to be suitable for further biological and medicinal studies. We therefore designed and synthesized two coumarin-tagged activity-based probes bearing the ebselen warhead. The heterodimers differ by the nature of the spacer structure, for which-in the second compound-a PEG/two-amide spacer was introduced. The interaction of this probe and of ebselen with two cysteine proteases was investigated.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5039496 | PMC |
| http://dx.doi.org/10.3390/ph9030043 | DOI Listing |
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