PT  - JOURNAL ARTICLE
AU  - Peng Chen
AU  - Hao Chen
AU  - Xinjie Zang
AU  - Min Chen
AU  - Haoran Jiang
AU  - Shasha Han
AU  - Xianggen Wu
TI  - Expression of Efflux Transporters in Human Ocular Tissues
AID  - 10.1124/dmd.113.052704
DP  - 2013 Nov 01
TA  - Drug Metabolism and Disposition
PG  - 1934--1948
VI  - 41
IP  - 11
4099  - http://dmd.aspetjournals.org/content/41/11/1934.short
4100  - http://dmd.aspetjournals.org/content/41/11/1934.full
SO  - Drug Metab Dispos2013 Nov 01; 41
AB  - To investigate the expression profiles of efflux transporters in human ocular tissues, quantitative real-time polymerase chain reaction, Western blotting, and immunohistochemistry were used to obtain the relative mRNA and protein expressions of various efflux transporters in human ocular tissues. The cornea, conjunctiva, iris-ciliary body (ICB), retina and choroid, human corneal epithelial cell line (HCEC), and human retinal pigment epithelial cell line (ARPE-19) were examined for the expressions of multidrug resistance–associated proteins 1–7 (MRP1–7), multidrug resistance 1 (MDR1) P-glycoprotein, lung resistance protein (LRP), and breast cancer–resistance protein (BCRP). The expression sites and patterns of efflux transporters were significantly different in ocular tissues, HCEC, and ARPE-19, as well as the expression profiles of efflux transporters in mRNA and protein levels in ocular tissues. At the protein level, MRP1-7, MDR1, and LRP were expressed in the corneal epithelium; MRP1-7, MDR1, LRP, and BCRP were expressed in the conjunctival epithelium; MRP1-2, MRP6-7, MDR1, and LRP were expressed in the ICB; MRP1-3, MRP6-7, MDR1, and LRP were expressed in the retina; MRP1-3, MRP6-7, MDR1, and LRP were expressed in the HCEC; and MRP7, MDR1, LRP, and BCRP were expressed in the ARPE-19. This quantitative and systematic study of efflux transporters in normal ocular tissues and cell lines provides evidence of cross-ocular tissue transporter expression differences, implying that efflux transporter expression variability should be taken into consideration for better understanding of ocular pharmacokinetic and pharmacodynamic data.