Thus, a PBPK model with the incorporation of in vitro MDR1 and BCRP transporter function data and transporter protein expression levels has been developed. As such, it is crucial to generate MDR1 and BCRP substrate data with a high fidelity. In this study, two widely use human MDR1 cell ...
几种ATP依赖的(ATP-BindingCassette,ABC)转运体超家族包括:多药耐药蛋白(MDR1/P-glycoprotein)、乳腺癌耐药蛋白(BCRP)及几种多药耐药联合蛋白家族(MRP)在这些屏障组织中都有高表达,它们在药物体内分布中的重要作用不容争议。 单层膜上皮细胞模型经常被用于研究ABC外排转运体在药物分布中的作用,其中一个常用的细胞...
BCRP)等,MDCK—MDR1 细胞高表达目的蛋白P—gP, 可以排除这些干扰,专一地鉴定P—gP 在药物外排中 的作用,筛选它的底物及抑制剂,所以在许多研究中 用它的单细胞层来检测P—gP 底物和抑制剂的活性. Brayden 等用MDCK.MDR1 和MDCK—MRP 细胞 模型研究了阿弗菌素与P—gP 和MRP 的相互作用, 药学学报...
Keywords:MDCK—MDR1cell;P—glycoprotein;drugtransport;cellmod el 膜转运蛋白对药物的吸收,排泄及代谢,起着 至关重要的作用.它可以保护细胞免受外来毒性物 质侵害.将哺乳动物肿瘤细胞暴露在一种细胞毒类 药物中一段时间后,这些细胞可通过降低胞内药物
本发明公开了一种MDCK-MDR1的药物吸收筛选体系及其构建方法，针对MDCK细胞中犬P-gp基因设计出了sgRNA ，将设计的sgRNA序列合成Oligo，构建sgRNA表达载体；将人源MDR1基因转染至MDCK-KO细胞中，筛选扩大阳性单克隆；蛋白免疫印迹法检测p-gp蛋白表达，成功表达者即表示MDCK-MDR1的药物吸收筛选体系构建成功。本发明基于...
It is of great challenge to predict human brain penetration for substrates of multidrug resistance protein 1 (MDR1) and/or breast cancer resistance protein (BCRP), two major efflux transporters at blood-brain barrier. Thus, a PBPK model with the incorporation of in vitro MDR1 and BCRP transpor...
MDCKII/MDCKII-BCRP细胞模型用于治疗胎儿快速性心律失常系列药物的跨胎盘转运机制的研究 研究治疗胎儿快速性心律失常的一系列药物在过表达乳腺癌耐药蛋白(breast cancer resistance protein,BCRP)的马丁达比犬肾上皮细胞系MDCKII-BCRP单层细胞模型中的跨膜... 王微,赵佳佳,王婷,... - 《药学学报》 被引量: 1发表...
The three most notable ABC transporters in cancer are MDR1, MRP1 and BCRP. Bcrp were not found expressed in MDCK I cells (data not shown), however, Mdr1 and Mrp1 were up-regulated during hyperosmolality. Hyperosmolality related to the increase of the oncotic pressure in solid cancer could...
Placenta ABCG2 (BCRP) Transport Rabbit Developmental toxicity Pesticides 1. Introduction Pesticides are used in conventional agriculture to manage weeds, insects or fungi while non-agricultural pesticides (biocides) have a wider range of applications as disinfectants, preservatives, and in pest control....
在检测外排转运蛋白BCRP抑制剂Ko143(5 μmol/L)对ACT001在MDCK-BCRP/Caco-2细胞单层上转运的影响和P-gp抑制剂维拉帕米(30 μmol/L)对ACT001在MDCK-MDR1/Caco-2细胞单层上转运的影响时,用同时含有抑制剂和药物的给药液代替只含药物的给药液即可。ACT001的给药浓度为3、30 μmol/L。每个浓度重复3次。用LC-...