Involvement of organic anion-transporting polypeptides and organic cation transporter in the hepatic uptake of jatrorrhizine

Liang, Ruifeng; Ge, Wenjing; Song, Xian-Mei; Zhang, Junping; Wei-feng, Cui; Zhang, She-Feng; Geng-sheng, LI

doi:10.1080/00498254.2019.1651921

Cited by 6 publications

(2 citation statements)

References 34 publications

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“…57,58 Prazosin is an inhibitor of OCT1. 56,59 Procainamide is an inhibitor of OCT2 with little effect on OCT1. 56,60 A wide range of inhibitor concentrations were tested due to the large reported variability in the effective inhibitory concentration.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…To reveal the relationship of the OCTs with lapatinib and afatinib, several inhibitors were chosen for their known transporter effects against OCTs. Corticosterone is a potent inhibitor of OCT3 with some inhibition of OCT1 and OCT2. , Verapamil has been implicated as an inhibitor of OCT1 , but can also act as an ABCB1 efflux inhibitor. , Prazosin is an inhibitor of OCT1. , Procainamide is an inhibitor of OCT2 with little effect on OCT1. , A wide range of inhibitor concentrations were tested due to the large reported variability in the effective inhibitory concentration. After preincubating A549 cell lines with transporter inhibitors, we dosed these cells with TKIs (lapatinib or afatinib) to test the effects of transporter inhibitors on the transport of TKI into cells.…”

Section: Resultsmentioning

confidence: 99%

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Facilitated Transport of EGFR Inhibitors Plays an Important Role in Their Cellular Uptake

Wong,

Dunnington,

et al. 2024

Anal. Chem.

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Epidermal growth factor receptor (EGFR) is a transmembrane protein commonly targeted by tyrosine kinase inhibitors (TKIs) as a front-line therapy for patients with many cancers including nonsmall cell lung cancer (NSCLC). Effective treatment requires efficient intracellular drug uptake and target binding. However, despite the recent success in the development of new TKI drugs, the mechanisms of uptake for many TKIs are still poorly understood due to the difficulty in imaging and measuring nonfluorescent drug molecules at a subcellular resolution. It has previously been shown that weakly basic TKI drugs are sequestered in lysosomes. Leveraging this property, we apply hyperspectral stimulated Raman scattering imaging to directly visualize and quantify two Food and Drug Administration-approved EGFR inhibitor drugs (lapatinib and afatinib) inside living cells and the changes in their cellular uptake upon the addition of organic cation transporter inhibitors. These single-cell quantitative measurements provide new insight into the role of membrane transporters in the uptake of TKI drugs in living cells.

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