A RETINOIC ACID RECEPTOR-ALPHA ANTAGONIST SELECTIVELY COUNTERACTS RETINOIC ACID EFFECTS

被引:264
作者
APFEL, C [1 ]
BAUER, F [1 ]
CRETTAZ, M [1 ]
FORNI, L [1 ]
KAMBER, M [1 ]
KAUFMANN, F [1 ]
LEMOTTE, P [1 ]
PIRSON, W [1 ]
KLAUS, M [1 ]
机构
[1] F HOFFMANN LA ROCHE & CO LTD, DIV PHARMA, CH-4002 BASEL, SWITZERLAND
关键词
RETINOIDS; CELL DIFFERENTIATION; HL-60; LYMPHOCYTES-B;
D O I
10.1073/pnas.89.15.7129
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Retinoic acid (RA) exerts its pleiotropic effects on cell growth and differentiation through the activation of a family of transcription factors-the RA receptors (RARs). Three subtypes of these receptors exist, RAR-alpha, RAR-beta, and RAR-gamma. The receptors are differentially expressed in different cell types and stages of development, suggesting that they may regulate different sets of genes. We have identified a synthetic retinoid with the characteristics of a selective RAR-alpha antagonist. This antagonist counteracts RA effects on HL-60 cell differentiation and on B-lymphocyte polyclonal activation. Beyond its potential practical relevance, this and other specific antagonists will be useful to dissect the RAR system and to assign to one given receptor each of the many RA-regulated functions.
引用
收藏
页码:7129 / 7133
页数:5
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