MDR1 synonymous polymorphisms alter transporter specificity and protein stability in a stable epithelial monolayer.

@article{Fung2014MDR1SP,
  title={MDR1 synonymous polymorphisms alter transporter specificity and protein stability in a stable epithelial monolayer.},
  author={King Leung Fung and James Lin-ko Pan and Shinobu Ohnuma and Paul E. Lund and Jessica N. Pixley and Chava Kimchi-Sarfaty and Suresh V Ambudkar and Michael M. Gottesman},
  journal={Cancer research},
  year={2014},
  volume={74 2},
  pages={598-608}
}
The drug efflux function of P-glycoprotein (P-gp) encoded by MDR1 can be influenced by genetic polymorphisms, including two synonymous changes in the coding region of MDR1. Here we report that the conformation of P-gp and its drug efflux activity can be altered by synonymous polymorphisms in stable epithelial monolayers expressing P-gp. Several cell lines with similar MDR1 DNA copy number were developed and termed LLC-MDR1-WT (expresses wild-type P-gp), LLC-MDR1-3H (expresses common haplotype P… CONTINUE READING
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