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首页> 外文期刊>Toxicology Letters: An International Journal Providing a Forum for Original and Pertinent Contributions in Toxicology Research >Radioligand binding assay for accurate determination of nuclear retinoid X receptors: A case of triorganotin endocrine disrupting ligands
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Radioligand binding assay for accurate determination of nuclear retinoid X receptors: A case of triorganotin endocrine disrupting ligands

机译：用于精确测定核视黄醇X受体的放射性配体结合测定：Trirogralotin内分泌破坏配体的情况

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摘要

Nuclear 9-cis retinoic acid receptors (retinoid X receptors, RXR) are promiscuous dimerization partners for a number of nuclear receptors. In the present study, we established a novel in vitro method for quantitative determination of the nuclear retinoid X receptors in rat liver. One type of high affinity and limited capacity RXR specific binding sites with the K-a value ranging from 1.011 to 1.727 x 10(9) l/mol and the B-max value ranging from 0.346 to 0.567 pmol/mg, was demonstrated. Maximal 9-cis retinoic acid (9cRA) specific binding to nuclear retinoid X receptors was achieved at 20 degrees C, and the optimal incubation time for the 9cRA-RXR complex formation was 120 min. From a number of endocrine disruptors, tributyltins and triphenyltins are known as RXR ligands. Our data confirmed the property of tributyltin chloride or triphenyltin chloride to bind to a high affinity and limited capacity RXR binding sites. Described optimal conditions for ligand binding to RXR molecules enabled us to calculate maximal binding capacity (Bmax) and affinity (Ka) values. This study provides an original RXR radioligand binding assay that can be employed for investigation of novel RXR ligands that comprise both drugs and endocrine disruptors. (C) 2016 Elsevier Ireland Ltd. All rights reserved.
机译：核9-CIS视黄酸受体（视网膜X受体，RXR）是许多核受体的混杂二聚化伴侣。在本研究中，我们建立了一种新的体外方法，用于定量测定大鼠肝脏核视网膜X受体的定量测定。一种类型的高亲和力和有限的容量RxR特异性结合位点，k-a值范围为1.011至1.727×10（9）L / mol和从0.346至0.567pmol / mg的B-max值。最大9-CIS视黄酸（9CRA）与核视黄醇X受体的特异性结合在20℃下实现，并且9CRA-RXR复合物形成的最佳孵育时间为120分钟。从许多内分泌破坏剂，致法和三苯基菌称为RXR配体。我们的数据证实了氯化丁蛋白或三苯基氯化锡的性质与高亲和力和有限的容量RXR结合位点结合。描述了与RXR分子结合的配体结合的最佳条件使我们能够计算最大结合能力（BMAX）和亲和力（KA）值。该研究提供了一种原始的RXR放射性配体结合测定，可用于研究新的RXR配体，其包含药物和内分泌破坏剂。 （c）2016 Elsevier Ireland Ltd.保留所有权利。

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