首页   按字顺浏览 期刊浏览 卷期浏览 Differentiation of F9 Embryonal Carcinoma Cells by Synthetic Retinoids: Amplitude of Pl...
Differentiation of F9 Embryonal Carcinoma Cells by Synthetic Retinoids: Amplitude of Plasminogen Activator Production Does Not Depend on Retinoid Potency or Affinity for F9 Nuclear Retinoic Acid Receptors

 

作者: J. Bailly,   C. Delescluse,   J.M. Bernardon,   B. Charpentier,   B. Martin,   W.R. Pilgrim,   B. Shroot,   M. Darmon,  

 

期刊: Skin Pharmacology and Physiology  (Karger Available online 1990)
卷期: Volume 3, issue 4  

页码: 256-267

 

ISSN:1660-5527

 

年代: 1990

 

DOI:10.1159/000210878

 

出版商: S. Karger AG

 

关键词: Retinoids;Potency;Retinoic acid receptors;F9 embryonal carcinoma cells;Plasminogen activator;Amplitude

 

数据来源: Karger

 

摘要:

Retinoic acid and analogues (retinoids) are able to induce the differentiation of F9 murine embryonal carcinoma stem cells into endoderm-like cells. The secretion of plasminogen activator (PA) which accompanies this differentiation is a good index of the biological response of F9 cells to retinoids. We have previously reported that the potency of a series of natural and synthetic retinoids, evaluated by the concentration which provokes half-maximal induction of PA, correlates well with the affinity of these compounds for the endogenous F9 nuclear retinoic acid receptors, but not for the cytosolic retinoic acid binding protein, CRABP. In this paper we show that various retinoids differ, not only in terms of potency, i.e. the dilution at which they are active, but also in terms of the amount of PA that they induce. This parameter, called amplitude, is used to quantify the extent of PA induction by a given retinoid relative to retinoic acid. The amplitude parameters of synthetic retinoids are found to vary over a wide range and are independent of both potency and binding affinity for F9 retinoic acid receptors. It is proposed that the amplitude of the biological response to a given retinoid is the resultant of three factors: (i) the total or partial agonist character of the retinoid; (ii) the binding spectrum of the retinoid for the various types of retinoic acid receptors; (iii) the chemical and metabolic stability of the retinoid in the test system.

 

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