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首页> 外文期刊>FEMS Microbiology Letters >Characterisation of human steroid hormone transport mediated by Cdrlp, a multidrug transporter of Candida albicans, belonging to the ATP binding cassette super family
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Characterisation of human steroid hormone transport mediated by Cdrlp, a multidrug transporter of Candida albicans, belonging to the ATP binding cassette super family

机译：Cdrlp介导的人类固醇激素转运的表征，Cdrlp是白色念珠菌的多药转运蛋白，属于ATP结合盒超家族

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摘要

Cdr1p, a multidrug transporter from a pathogenic yeast Candida albicans, confers resistance to several unrelated drugs including anti-Candida drugs. We demonstrate that Cdr1p can specifically transport human steroid hormones namely beta-estradiol and corticosterone. Saccharomyces cerevisiae transformant S-12, harbouring the CDR1 gene, accumulated about 3-fold less [H-3]beta-estradiol and about 2-fold less [H-3]corticosterone than the non-transformed strain. When CDR1 was expressed in AD strain (AD-CDR1) which had seven ATP binding cassette (ABC) superfamily of putative transporter genes disrupted, the net accumulation of these hormones as compared to S-12 was significantly lower. Efflux of P-estradiol and corticosterone was inhibited by a 100-fold higher (200 nM) concentration of beta-estradiol, corticosterone, ergosterol or dexamethasone, but progesterone which could not be transported by Cdr1p did not affect the efflux and thus accumulation. Interestingly, some of the drugs viz. cycloheximide, chloramphenicol, fluconazole and o-phenanthroline, to which CDR1 confers resistance, could also prevent efflux and enhance accumulation to some extent. In conclusion, we show that human steroid hormones could be the substrates for Cdr1p and the energy dependent transport mediated by it is specific for estradiol and corticosterone. (C) 1998 Published by Elsevier Science B.V. All rights reserved. [References: 25]
机译：Cdr1p是一种来自致病性酵母白色念珠菌的多药转运蛋白，可赋予对几种不相关药物的抗性，包括抗Candida药物。我们证明，Cdr1p可以特异性转运人类类固醇激素，即β-雌二醇和皮质酮。带有CDR1基因的啤酒酵母转化子S-12积累的[H-3]β-雌二醇比未转化菌株少约3倍，[H-3]皮质酮少约2倍。当CDR1在具有七个推定转运蛋白基因的ATP结合盒（ABC）超家族被破坏的AD菌株（AD-CDR1）中表达时，与S-12相比，这些激素的净积累显着降低。 β-雌二醇，皮质酮，麦角固醇或地塞米松的浓度高100倍（200 nM），可抑制P-雌二醇和皮质酮的流出，但Cdr1p不能转运的孕酮不会影响其流出并因此积累。有趣的是，有些药物也可以。 CDR1具有耐药性的环己酰亚胺，氯霉素，氟康唑和邻菲咯啉也可以防止外排并在一定程度上增强积累。总之，我们表明人类固醇激素可能是Cdr1p的底物，其介导的能量依赖性转运对雌二醇和皮质酮具有特异性。 （C）1998，Elsevier Science B.V.保留所有权利。 [参考：25]

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