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Titolo:
First non-radioactive assay for in vitro screening of histone deacetylase inhibitors
Autore:
Hoffmann, K; Brosch, G; Loidl, P; Jung, M;
Indirizzi:
Univ Munster, Dept Pharmaceut Chem, D-48149 Munster, Germany Univ MunsterMunster Germany D-48149 ceut Chem, D-48149 Munster, Germany Innsbruck Univ, Sch Med, Dept Microbiol, A-6020 Innsbruck, Austria Innsbruck Univ Innsbruck Austria A-6020 obiol, A-6020 Innsbruck, Austria
Titolo Testata:
PHARMAZIE
fascicolo: 8, volume: 55, anno: 2000,
pagine: 601 - 606
SICI:
0031-7144(200008)55:8<601:FNAFIV>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSFORMED-CELL DIFFERENTIATION; TRICHOSTATIN-A; INDUCERS; ACETYLATION; TRAPOXIN; COMPLEX; ANALOGS; HD2;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
25
Recensione:
Indirizzi per estratti:
Indirizzo: Jung, M Univ Munster, Dept Pharmaceut Chem, Hittorfstr 58-62, D-48149 Munster, Germany Univ Munster Hittorfstr 58-62 Munster Germany D-48149 er, Germany
Citazione:
K. Hoffmann et al., "First non-radioactive assay for in vitro screening of histone deacetylase inhibitors", PHARMAZIE, 55(8), 2000, pp. 601-606

Abstract

Inhibitors of histone deacetylase (HD) are of great potential as new drugsdue to their ability to influence transcriptional regulation and to induceapoptosis or differentiation in cancer cells. So far only radioactive enzyme activity assays or in vivo assays with subsequent electrophoresis and immunoblotting existed to study the activity of HD and potential inhibitors. To aid in the search of new inhibitors, a non-radioactive screening assay was sought and we have previously succeeded in establishing this for the first time. The assay uses an aminocoumarin derivative of an Omega-acetylated lysine as substrate for the enzyme. Here we report full experimental details, the evaluation of other potential substrates, and comparative analysis of various inhibitors. This advantageous method should have an impact on further developments in the field.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/11/18 alle ore 04:36:05