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Titolo:
Establishment of a high-throughput screening system for caspase-3 inhibitors
Autore:
Park, SY; Park, SH; Lee, IS; Kong, JY;
Indirizzi:
Korea Res Inst Chem Technol, Pharmaceut Screening Res Lab, Taejon 305600, South Korea Korea Res Inst Chem Technol Taejon South Korea 305600 05600, South Korea Konkuk Univ, Dept Vet Med, Seoul 143701, South Korea Konkuk Univ Seoul South Korea 143701 Vet Med, Seoul 143701, South Korea
Titolo Testata:
ARCHIVES OF PHARMACAL RESEARCH
fascicolo: 3, volume: 23, anno: 2000,
pagine: 246 - 251
SICI:
0253-6269(200006)23:3<246:EOAHSS>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
INTERLEUKIN-1-BETA CONVERTING-ENZYME; ICE/CED-3 PROTEASE; FAMILY PROTEASES; POTENTIAL ROLE; CELL-DEATH; APOPTOSIS; DISEASE; MEDIATOR; CLEAVAGE; DAMAGE;
Keywords:
apoptosis; caspase-3; high throughput screening;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Kong, JY Korea Res Inst Chem Technol, Pharmaceut Screening Res Lab, 100 Jang Dong, Taejon 305600, South Korea Korea Res Inst Chem Technol 100 Jang Dong Taejon South Korea 305600
Citazione:
S.Y. Park et al., "Establishment of a high-throughput screening system for caspase-3 inhibitors", ARCH PH RES, 23(3), 2000, pp. 246-251

Abstract

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 asan effect molecule to proteolytically cleave intracellular substrates thatare 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 or 20 mu M.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/20 alle ore 00:05:47