Efflux transporters facilitate the export of compounds from the cell, both in some cellular assays, also in ADME studies. These transporters belong to the ATP-binding cassette (ABC) family. P-glycoprotein (Pgp) is one of the most widely known efflux transporter which has a great effect on the success of some drug discovery projects. Pgp is a 170 KD protein with 1280 amino acids and 12 trans-membrane segments, expressed by gene known as MDR1 or ABCB1.
ICE Bioscience generated MDCKII-MDR1 cell line in house by lentiviral system in-house, also developed permeability assay in both parental MDCKII and MDCKII-MDR1 cells. As there is some basic transportation activity in wildtype cell line, currently we are constructing MDCKII-KO-Pgp cell line to support substrate identification study, other transporters expression cell lines are also under validation now, we could also generate Pgp overexpression cell line in cellular screening assay to evaluate efflux effect of some compounds.
Commercial Instruments and Products for the Measurement of Permeability
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