piroxicam has been researched along with ebselen* in 2 studies
2 other study(ies) available for piroxicam and ebselen
| Article | Year |
|---|---|
Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
Cumulative evidence suggests that β-amyloid and oxidative stress are closely related with each other and play key roles in the process of Alzheimer's disease (AD). Multitarget regulation of both pathways might represent a promising therapeutic strategy. Here, a series of selenium-containing compounds based on ebselen and verubecestat were designed and synthesized. Biological evaluation showed that 13f exhibited good BACE-1 inhibitory activity (IC Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid Precursor Protein Secretases; Antioxidants; Aspartic Acid Endopeptidases; Azoles; Binding Sites; Blood-Brain Barrier; Cyclic S-Oxides; Drug Design; Humans; Interleukin-6; Isoindoles; Ligands; Mitochondria; Molecular Docking Simulation; Neuroprotective Agents; NF-E2-Related Factor 2; Organoselenium Compounds; Oxidative Stress; Peptide Fragments; Reactive Oxygen Species; Selenium; Signal Transduction; Thiadiazines | 2021 |
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
Given their medical importance, proteases have been studied by diverse approaches and screened for small molecule protease inhibitors. Here, we present a multiplexed microsphere-based protease assay that uses high-throughput flow cytometry to screen for inhibitors of the light chain protease of botulinum neurotoxin type A (BoNTALC). Our assay uses a full-length substrate and several deletion mutants screened in parallel to identify small molecule inhibitors. The use of multiplex flow cytometry has the advantage of using full-length substrates, which contain already identified distal-binding elements for the BoNTALC, and could lead to a new class of BoNTALC inhibitors. In this study, we have screened 880 off patent drugs and bioavailable compounds to identify ebselen as an in vitro inhibitor of BoNTALC. This discovery demonstrates the validity of our microsphere-based approach and illustrates its potential for high-throughput screening for inhibitors of proteases in general. Topics: Antigens, Bacterial; Azoles; Bacterial Toxins; Botulinum Toxins, Type A; Drug Evaluation, Preclinical; Flow Cytometry; Fluorescence Resonance Energy Transfer; High-Throughput Screening Assays; Isoindoles; Metalloproteases; Microspheres; Organoselenium Compounds; Protease Inhibitors | 2010 |