• Title/Summary/Keyword: chemical screening

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Establishment of a High-Throughput Screening System for Caspase-3 Inhibitors

  • Park, Seung-Yong;Park, Song-Hee;Lee, Il-Sun;Kong, Jae-Yang
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.246-251
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    • 2000

  • In most tissues, apoptosis plays a pivotal role in normal development and for regulating cell number, thus inappropriate apoptosis underlies a variety of diseases. Caspase-3 is one of a family of caspases that are mainly involved in the apoptotic signal transduction pathway, where caspase-3 acts as an effect molecule to proteolytically cleave intracellular substrates that are necessary for maintaining cell survival. Recent evidences show that apoptotic cell death can be blocked by inhibiting caspase-3, suggesting its inhibitors have potential to be therapeutic drugs for the diseases related with inappropriate apoptosis. We have established a screening system to search caspase-3 inhibitors from chemical libraries stocked in our institute. The enzyme assay is configured entirely in 96-well format, which is easily adapted for high throughput screening. Before performing mass screening, 80 in-house compounds were screened as a preliminary experiment, and we found that morin hydrate inhibited caspase-3 by 66.4 % at the final concentration of 20 ${\mu}g/m{\ell}$.

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