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Selective Synthetic Ligands for Human Nuclear Retinoic Acid Receptors

 

作者: Bernard Martin,   Jean-Michel Bernardon,   Marie-Thérèse Cavey,   Bruno Bernard,   Isabelle Carlavan,   Bruno Charpentier,   William R. Pilgrim,   Braham Shroot,   Uwe Reichert,  

 

期刊: Skin Pharmacology and Physiology  （Karger Available online 1992）
卷期: Volume 5, issue 1  

页码: 57-65

 

ISSN:1660-5527

 

年代: 1992

 

DOI:10.1159/000211018

 

出版商: S. Karger AG

 

关键词: Retinoic acid receptors;Selective ligands;Plasminogen activator

 

数据来源: Karger

 

摘要:

From a series of naphthalene and benzoic acid derivatives we have identified synthetic retinoic acid analogues exhibiting high selectivity for the nuclear retinoic acid receptors RARα (Am 580), RARβ (CD 2019) and RARγ (CD 437) as well as ligands sharing high affinities for all RAR subtypes (CD 367). The compounds were evaluated in two complementary screening systems: (1) binding to nuclear proteins extracted from COS-7 cells after transfection with the appropriate expression vectors, and (2) induction of plasminogen activator in the embryonic mouse teratocarcinoma cell line F9. All compounds behaved as retinoic acid agonists in the F9 te

 

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