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Inter-Individual and Regional Variability in Drug Transporter Abundance at the Human Blood-Brain Barrier Measured by Quantitative Targeted Proteomics.
Clinical Pharmacology and Therapeutics 2019 January 24
For in-vitro to in-vivo extrapolation (IVIVE) of brain distribution of drugs that are transported at the human blood-brain barrier (BBB), it's important to quantify the inter-individual and regional variability of drug transporter abundance at this barrier. Therefore, using quantitative targeted proteomics, we compared the abundance of ABC and SLC transporters in brain microvascular endothelial cells (BMEC) isolated from post-mortem specimens of two matched brain regions, the occipital (BA17) and parietal (BA39) lobe, from 30 adults. Of the quantifiable transporters, the abundance ranked: GLUT1>BCRP>P-gp>ENT1>OATP2B1. The abundance of MRP1/2/3/4, OATP1A2, OAT3, OCT1/2, OCTN1/2, or ENT2 was below the limit of quantification. Transporter abundance per g of tissue (scaled using GLUT1 abundance in BMEC vs. brain homogenate) in BA17 was 30-42% higher than BA39. The inter-individual variability in transporter abundance (%CV) was 35-57% (BA17) and 27-46% (BA39). These data can be used in proteomics-informed bottom-up IVIVE to predict human brain drug distribution. This article is protected by copyright. All rights reserved.
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