In vivo biological activity of retinoids partially correlates to their affinity to recombinant retinoic-acid receptor alpha and recombinant-cellular retinoic-acid-binding protein I.

In vivo biological activity of retinoids partially correlates to their affinity to recombinant retinoic-acid receptor alpha and recombinant-cellular retinoic-acid-binding protein I.
复制标题

类维生素A的体内生物活性部分与其对重组视黄酸受体α和重组细胞视黄酸结合蛋白I的亲和力相关。

DOI:
--
复制
发表时间:
1993
期刊:
European Journal of Biochemistry
影响因子:
--
通讯作者:
W. Mueller
W. Mueller
中科院分区:
--
文献类型:
--
作者:
S. Keidel;M. Szardenings;W. Mueller

文献摘要

参考文献

被引文献

相似文献

合成了几种已知的和一些新的维甲酸类化合物,并通过测定,基于在P19畸胎瘤细胞,人前列腺癌细胞和新生大鼠心脏细胞的原代培养物中诱导碱性磷酸酶来研究它们的体内活性。在这项研究中使用的测定被发现是可重复的,并用于快速筛选类维生素A的生物活性。两个新合成的化合物具有很高的生物活性。将化合物的生物学效力与其结合重组视黄酸受体α和通过Charsorb结合测定测定的细胞视黄酸结合蛋白I的能力进行比较。这两种视黄酸结合蛋白的mRNA可以检测到在三个细胞系的调查。正如从不同的视黄酸受体的数量所预期的那样,结果表明,类维生素A不需要结合视黄酸受体α或细胞视黄酸结合蛋白I以表现出生物活性,但大多数研究的类维生素A显示出与这些蛋白质的结合与其生物活性之间的明确相关性。
Several known and some new retinoids were synthesized and their in vivo activity was investigated by an assay, based on induction of alkaline phosphatase in P19 teratocarcinoma cells, human prostate carcinoma cells and primary cultures of neonatal rat heart cells. The assay used in this study was found to be reproducible and useful for rapid screening of retinoids for biological activity. Two newly synthesized compounds exhibit high biological activity. The biological potency of the compounds was compared to their ability to bind to recombinant retinoic-acid receptor alpha and to cellular retinoic-acid-binding protein I determined by Charsorb-binding assay. mRNA of both retinoic-acid-binding proteins could be detected in the three cell lines investigated. As expected from the number of different retinoic-acid receptors, the results suggest that retinoids do not need to bind retinoic-acid receptor alpha nor cellular retinoic-acid-binding protein I in order to exhibit biological activity, but most retinoids investigated show a clear correlation between binding to these proteins and their biological activity.
DOI: 10.1016/0162-3109(91)90055-4
发表时间: 1991
期刊: Immunopharmacology
影响因子: --
作者:
Orosz,CG;Zinn,NE;Bishop,DK;Leppink,DL;Faherty,D;Ferguson,RM
通讯作者: Ferguson,RM
F9胚胎癌细胞分化过程中视黄酸和视黄醇的代谢。
DOI: 10.1073/pnas.82.14.4658
发表时间: 1985
影响因子: 11.1
作者:
Williams,JB;Napoli,JL
通讯作者: Napoli,JL
鉴定具有核受体亚型选择性活性的类维生素A。
DOI: --
发表时间: 1991
期刊: Cancer research
影响因子: 11.2
作者:
Lehmann,JM;Dawson,MI;Hobbs,PD;Husmann,M;Pfahl,M
通讯作者: Pfahl,M
DOI: 10.1056/nejm199009203231205
发表时间: 1990-09-20
影响因子: 158.5
作者:
HONG, WK;LIPPMAN, SM;GOEPFERT, H
通讯作者: GOEPFERT, H