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Titolo:
RETINOID ANTAGONISTS
Autore:
UMEMIYA H; KAGECHIKA H; FUKASAWA H; HASHIMOTO Y; SHUDO K;
Indirizzi:
UNIV TOKYO,FAC PHARMACEUT SCI,BUNKYO KU,7-3-1 HONGO TOKYO 113 JAPAN UNIV TOKYO,FAC PHARMACEUT SCI,BUNKYO KU TOKYO 113 JAPAN UNIV TOKYO,INST MOL & CELLULAR BIOSCI,BUNKYO KU TOKYO 113 JAPAN
Titolo Testata:
Yakugaku zasshi
fascicolo: 12, volume: 116, anno: 1996,
pagine: 928 - 941
SICI:
0031-6903(1996)116:12<928:RA>2.0.ZU;2-D
Fonte:
ISI
Lingua:
JPN
Soggetto:
RECEPTOR-SELECTIVE RETINOIDS; LIGAND-BINDING DOMAIN; LEUKEMIA-CELLS HL-60; ACID RECEPTOR; RETINOBENZOIC ACIDS; HETEROCYCLIC RING; CRYSTAL-STRUCTURE; ALPHA; RXR; DIFFERENTIATION;
Keywords:
RETINOIC ACID; RETINOID; ANTAGONIST; SYNERGIST; NUCLEAR RECEPTOR;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
H. Umemiya et al., "RETINOID ANTAGONISTS", Yakugaku zasshi, 116(12), 1996, pp. 928-941

Abstract

Retinoids, retinoic acid and its bioisosters, regulate many biological functions such as cell differentiation, proliferation and embryonic development in vertebrates, through binding to and activating their specific nuclear receptors. There are two classes of nuclear receptors for retinoids, retinoic acid receptors (RAR alpha, beta, gamma) and retinoid X receptors (RXR alpha, beta, gamma). Several retinoid antagonists, which bind to but not activate RARs, have been reported. Among them, lbenzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid (LE135, 20)is a RAR beta-selective retinoid antagonist. Structure-activity relationships of LE135 (20) showed that the naphthalenyl analogs [LE540 (21) and LE550 (22)] are more potent retinoid antagonists in HL-60 assay. Contrary to the antagonistic activity of LE135 (20), an isomer of LE135 (20), )-5-methyldibenzo-[b,e][1,4]diazepin-11-yl)benzoic acid (HX600, 39) enhanced the activities of retinoids. Although the synergistic activity of HX600 (39) can be explained by the binding to RXRs and thefurther activation of RAR/RXR heterodimer activated by retinoid (RAR ligand), the significantly different biological character of HX600 (39) from the typical RXR-selective ligand suggested the possibility of the participation of other nuclear receptors or cofactors in the retinoid synergism.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/01/20 alle ore 16:56:07