Indeed, overexpression of efflux ABC transporters in cancer cells or bacteria limits drug exposure and causes therapeutic failure that is known as multidrug resistance (MDR). With the discovery of functional noncoding microRNAs (miRNAs) produced from the genome, many miRNAs ha...
将细胞接种在Transwell小室上,培养至形成完整的极化细胞单层,通过开展双向渗透性实验(顶端到基底端(apical‑basolateral,A-B)和B-A方向),并在含有或不含特定ABC转运体抑制剂的条件下,进行双向表观渗透系数(apparent permeability coefficient,Papp)以及外排率(efflux ratio,ER)的计算,评价化合物是否为该ABC转运体...
efflux transporters provide neuroprotection against several neurotoxins.ABC efflux transporters contribute to the pharmacoresistance against CNS drugs.Several stressors modulate the activity of ABC efflux transporters at BBB.Pathological alterations of ABC efflux transporters are associated with many CNS ...
Indeed, overexpression of efflux ABC transporters in cancer cells or bacteria limits drug exposure and causes therapeutic failure that is known as multidrug resistance (MDR). With the discovery of functional noncoding microRNAs (miRNAs) produced from the genome, many miRNAs have been revealed to ...
将细胞接种在Transwell小室上,培养至形成完整的极化细胞单层,将受试药物添加到单层细胞的顶端(apical,AP)或基底侧(basolateral,BL),测量渗透入接收室中的药量,根据AP→BL(吸收)和BL→AP(流出)两个方向上的表观渗透系数(apparent permeability coefficient,Papp)计算外排率(efflux ratio,ER),评价化合物是否为该ABC...
(heme efflux)[128], in renal urate efflux[129], or in the placenta[122]. ABCG2 is a key determinant of thepharmacokinetics(intestinal absorption and hepatic elimination)[15]of drugs (e.g., rosuvastatin), and can be involved in DDI[2]. Hence, ABCG2 is recommended to be investigated ...
Multidrug transporter proteins are best known for their contributions to chemoresistance through the efflux of anticancer drugs from cancer cells. However, a considerable body of evidence also points to their importance in cancer extending beyond drug transport to fundamental roles in tumour biology. Curr...
ATP-binding cassette (ABC) transporters are efflux transporters found in all organisms. These proteins are responsible for pumping xenobiotic and endogenous metabolites through extra- and intracellular membranes, thereby reducing cellular concentrations of toxic compounds. ABC transporters have been associated...
In this review, we provide an overview of the role of ABC efflux transporters in MDR and pharmacokinetics. Preclinical assays for the assessment of drug transport and development of MDR modulators are also discussed. 展开 关键词: Cancer therapy multidrug resistance ABC transporter pharmacokinetic Drug...
the ABC transporters are energy-dependent efflux transporters, which utilize ATP for their transport process to regulate the cellular levels of hormones, lipids, metabolites,xenobiotics, and other small molecules by pumping them out of the cells through the cell membrane[13]. All ABC transporters hav...