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Titolo:
Repression of androgen-regulated gene expression by dominant negative androgen receptors
Autore:
Bramlett, KS; Dits, NFJ; Sui, XM; Jorge, MC; Zhu, X; Jenster, G;
Indirizzi:
Erasmus Univ, Josephine Nefkens Inst, Dept Urol, NL-3000 DR Rotterdam, Netherlands Erasmus Univ Rotterdam Netherlands NL-3000 DR DR Rotterdam, Netherlands Univ Texas, MD Anderson Canc Ctr, Dept Urol, Houston, TX 77030 USA Univ Texas Houston TX USA 77030 anc Ctr, Dept Urol, Houston, TX 77030 USA
Titolo Testata:
MOLECULAR AND CELLULAR ENDOCRINOLOGY
fascicolo: 1-2, volume: 183, anno: 2001,
pagine: 19 - 28
SICI:
0303-7207(20011025)183:1-2<19:ROAGEB>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
ZINC-FINGER PROTEINS; N-TERMINAL DOMAIN; TRANSCRIPTIONAL REPRESSION; BINDING CHARACTERISTICS; PROSTATE-CANCER; LNCAP CELLS; ACTIVATION; DEACETYLASES; SUPERFAMILY; INHIBITION;
Keywords:
steroid receptor; histone deacetylase; transcription repression; transactivation; dominant negative mutant; steroid hormones;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Jenster, G Erasmus Univ, Josephine Nefkens Inst, Dept Urol, POB 1738, NL-3000 DR Rotterdam, Netherlands Erasmus Univ POB 1738 Rotterdam Netherlands NL-3000 DR erlands
Citazione:
K.S. Bramlett et al., "Repression of androgen-regulated gene expression by dominant negative androgen receptors", MOL C ENDOC, 183(1-2), 2001, pp. 19-28

Abstract

The androgen receptor (AR) is a ligand-dependent transcription activator responsible for male sexual development. In order to specifically inhibit the AR pathway, dominant negative ARs were constructed by inactivation of themajor transactivation domains of the wild type AR and fusing this mutant (AR122) to the Kruppel-associated box (KRAB) repressor domain and/or histonedeacetylase (HDAC1). The HDAC1-KRAB-AR122 protein was the most successful dominant negative AR, capable of repressing the wild type AR ninefold when co-expressed at a 1:1 plasmid ratio. A maximal repression of 41-fold was achieved when HDAC1-KRAB-AR122 was cotransfected with the wild type AR at a 4:1 plasmid ratio. HDAC1-KRAB-AR122 repressed transcription in a ligand-dependent manner since it inhibited a constitutively active AR mutant (AR5) only in the presence of agonists. High concentrations of partial agonists suchas RU486, cyproterone acetate, and estradiol were also capable of triggering repression by HDAC1-KRAB-AR122. The potent dominant negative AR proteinsmight prove useful tools to inhibit AR function in vitro and in vivo. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/10/20 alle ore 16:20:14