Your browser doesn't support javascript.
loading
Relationship between binding affinities to cellular retinoic acid-binding protein and in vivo and in vitro properties for 18 retinoids.
Cancer Res ; 40(2): 212-20, 1980 Feb.
Article em En | MEDLINE | ID: mdl-7188681
A new rapid assay has been developed for measurement of the binding of [3H]retinoic acid to cellular retinoic acid-binding protein. The assay, which uses activated charcoal for the separation of bound from unbound retinoic acid, was used to determine the concentration required to inhibit the binding of [3H]retinoic acid to cellular retinoic acid-binding protein by 50% for 18 retinoids with free carboxylic acid groups. Partially purified cellular retinoic acid-binding proteins isolated from rat testes and carcinogen-induced rat mammary tumors were used for these determinations. The following parameters were also determined for some or all of the retinoids: hypervitaminosis A doses; activity against carcinogen-induced mouse skin papillomas; inhibition of growth of a rat chondrosarcoma; inhibition of growth of 3T6 cells; and differentiation of the embryonal carcinoma cell line PCC4.azaIR. While all retinoids that are potent in these biological test systems bind tightly to cellular retinoic acid-binding protein, the converse is not true. The lack of a consistent quantitative correlation between 50% inhibitory concentration and biological activity is probably due to insufficient concentrations of the retinoid in the target tissue or celll, which is a consequence of factors such as absorbability, metabolism, tissue distribution, and pharmacokinetics.
Assuntos
Buscar no Google
Base de dados: MEDLINE Assunto principal: Tretinoína / Vitamina A / Proteínas de Ligação ao Retinol Limite: Animals Idioma: En Ano de publicação: 1980 Tipo de documento: Article
Buscar no Google
Base de dados: MEDLINE Assunto principal: Tretinoína / Vitamina A / Proteínas de Ligação ao Retinol Limite: Animals Idioma: En Ano de publicação: 1980 Tipo de documento: Article