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首页> 外文期刊>Drug metabolism letters >A comparative study of the CYP450 inhibition potential of marketed drugs using two fluorescence based assay platforms routinely used in the pharmaceutical industry.
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A comparative study of the CYP450 inhibition potential of marketed drugs using two fluorescence based assay platforms routinely used in the pharmaceutical industry.

机译:制药工业常规应用两种荧光的测定平台CYP450抑制潜力的比较研究。

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摘要

Semi-automated high throughput screening for the inhibition of major human cytochrome P450 enzymes (1A2, 2C9, 2C19, 2D6 and 3A4) expressed in Escherichia Coli (Cypex bactosomes) or human lymphoblastoid cells (Gentest cDNA microsomes) using fluorescent probes has been evaluated using 68 marketed drugs. In general lower IC50 values were obtained with Cypex bactosomes compared with Gentest cDNA microsomes. This could be due to use of higherconcentration of protein and also the lower activity of Gentest cDNA microsomes. Notably, when compared with in vivo clinical drug-drug interactions (cDDIs) gathered from clinical studies reported in the scientific literature Cypex bactosome data was better at predicting in vivo cDDI. Consequently, from the data obtained in this comparative study, a fluorescence based assay using Cypex bactosomes is more suitable as a front-line screen for the prediction of potential downstream CYP450 driven cDDIs.
机译:使用荧光探针(CoMex Bactosomes)或人淋巴细胞(Codest cDNA微粒)在大肠杆菌(Cypex Bactosomes)或使用荧光探针中表达的主要人细胞色素P450酶(1a2,2c9,2c19,2d6和3a4)的半自动高通量筛选已经使用荧光探针进行评估 68名销售药物。 通常,通过Cypex Bactosomes获得较低的下部IC 50值,与CDNA微粒体相比。 这可能是由于使用蛋白质的康复和较低的CDNA微粒瘤的较低活性。 值得注意的是,与体内临床药物 - 药物相互作用(CDDIS)相比,从科学文献Cypex Bactosome数据中报告的临床研究中收集的临床研究,更好地预测体内CDDI。 因此,从该比较研究中获得的数据,使用Cymex Bactosomes的荧光的测定更适合于预测潜在下游CYP450驱动CDDIS的前线屏幕。

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