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Titolo:
Development of peptide antagonists that target estrogen receptor-cofactor interactions
Autore:
McDonnell, DP; Chang, CY; Norris, JD;
Indirizzi:
Duke Univ, Med Ctr, Dept Pharmacol & Canc Biol, Durham, NC 27710 USA Duke Univ Durham NC USA 27710 Pharmacol & Canc Biol, Durham, NC 27710 USA
Titolo Testata:
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
fascicolo: 5, volume: 74, anno: 2000,
pagine: 327 - 335
SICI:
0960-0760(20001130)74:5<327:DOPATT>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
DISTINCT CONFORMATIONAL-CHANGES; DOMAIN-CONTAINING PROTEINS; NUCLEAR RECEPTOR; BREAST-CANCER; POSTMENOPAUSAL WOMEN; LIGAND TARGETS; CO-REPRESSOR; ER-ALPHA; TAMOXIFEN; HORMONE;
Keywords:
peptide antagonists; estrogen; receptor-cofactor interaction; transcriptional activity;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
47
Recensione:
Indirizzi per estratti:
Indirizzo: McDonnell, DP Duke Univ, Med Ctr, Dept Pharmacol & Canc Biol, Box 3813, Durham, NC 27710USA Duke Univ Box 3813 Durham NC USA 27710 , Durham, NC 27710USA
Citazione:
D.P. McDonnell et al., "Development of peptide antagonists that target estrogen receptor-cofactor interactions", J STEROID B, 74(5), 2000, pp. 327-335

Abstract

We have developed a series of high-affinity peptide antagonists that inhibit the transcriptional activity of both subtypes of the human estrogen receptor (ER alpha and ER beta). We believe that it will be possible to developthese peptides, or corresponding peptidomimetic derivatives, into pharmaceuticals for use in the treatment of breast cancer and other estrogenopathies. It is anticipated that drugs of this type could be used in combination with classical antiestrogens, such as tamoxifen, to achieve a complete blockage of ER-transcriptional activity. Although ER has been the primary targetof our studies to date, it is likely that the insights gained from this work will apply to other nuclear receptors and transcription factors. (C) 2000 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 12:48:35