Laboratory of Biotechnology and Applied Pharmacology, CNRS UMR8113, Ecole Normale Supérieure de Cachan, Cachan, France.
J Immunol Methods. 2011 Oct 28;373(1-2):229-39. doi: 10.1016/j.jim.2011.08.022. Epub 2011 Sep 3.
A cell-based assay has been developed for the quantification of the activity of TNFα antagonists based on human erythroleukemic K562 cells transfected with a NFκB regulated firefly luciferase reporter-gene construct. Both drug activity and anti-drug neutralizing antibodies can be quantified with a high degree of precision within 2h, and without interference from cytokines and other factors known to activate NFκB. The assay cells also contain the Renilla luciferase reporter gene under the control of a constitutive promoter that allows TNFα-induced firefly luciferase activity to be normalized relative to Renilla luciferase expression. Thus, results are independent of cell number or differences in cell viability, resulting in intra and inter assay coefficients of variation of 10% or less. Normalization of results relative to the expression of an internal standard also provides a means for correcting for serum matrix effects and allows residual drug levels or anti-drug neutralizing antibodies to be quantified even in serum samples with a relatively high degree of cytotoxicity.
已经开发出一种基于转染了 NFκB 调控的萤火虫荧光素酶报告基因构建体的人红白血病 K562 细胞的细胞测定法,用于定量 TNFα 拮抗剂的活性。药物活性和抗药物中和抗体都可以在 2 小时内以高精度定量,并且不受已知激活 NFκB 的细胞因子和其他因素的干扰。测定细胞还含有受组成型启动子控制的海肾荧光素酶报告基因,该基因允许相对于海肾荧光素酶表达来归一化 TNFα 诱导的萤火虫荧光素酶活性。因此,结果与细胞数量或细胞活力的差异无关,导致内和间测定的变异系数小于 10%。相对于内部标准的表达对结果进行归一化还提供了一种校正血清基质效应的方法,并允许即使在具有相对高细胞毒性的血清样本中也定量残留药物水平或抗药物中和抗体。