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The thyroid transporter OATP1C1, expressed in the choroid plexus and in astrocytes, is also a potential pharmacological target. Based on their established pharmacological relevance, screening the drug interaction profile of OATP1A2 and OATP1C1 is highly desirable. However, drug interaction screens require suitable model systems and functional assays. In the current study, uptake of a set of cell\u2010impermeable fluorescent dyes was screened in HEK\u2010293 and A431 cell lines overexpressing OATP1A2 and OATP1C1. Based on the uptake of fluorescent dye substrates, a functional assay was developed, which was used to characterize OATP inhibitors\/substrates. We identify Live\/Dead Green (LDG), Live\u2010or\u2010Dye 488, and sulforhodamines 101, G, and B as novel fluorescent substrates of OATP1A2 and OATP1C1. We show that LDG uptake is proportional to OATP1A2\/1C1 expression, allowing the isolation of cells expressing high transporter levels. Additionally, dye uptake can be used to characterize the drug interaction pattern of OATP1A2 and OATP1C1. We demonstrate that third\u2010generation P\u2010glycoprotein inhibitors elacridar, tariquidar, and zosuquidar inhibit OATP1A2 function. Increased toxicity of elacridar in OATP1A2\u2010expressing cells suggests that OATP1A2 may modulate the distribution of this compound. The fluorescence\u2010based assays developed in the current study are a good alternative of radioligand\u2010based tests and pave the way toward high\u2010throughput screens for OATP1A2\/1C1 drug interaction studies.<\/jats:p>","DOI":"10.1111\/febs.15156","type":"journal-article","created":{"date-parts":[[2019,11,26]],"date-time":"2019-11-26T16:39:27Z","timestamp":1574786367000},"page":"2468-2485","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":30,"title":["A novel fluorescence\u2010based functional assay for human OATP1A2 and OATP1C1 identifies interaction between third\u2010generation P\u2010gp inhibitors and OATP1A2"],"prefix":"10.1111","volume":"287","author":[{"given":"\u00c9va","family":"Bakos","sequence":"first","affiliation":[{"name":"Membrane Protein Research Group Institute of Enzymology Research Centre for Natural Sciences Hungarian Academy of Sciences Budapest 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