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Dissertation/Thesis Abstract

Drug interactions with the human organic anion transporter 3, OAT3
by Munns, Denton R., M.S., University of California, San Francisco, 2009, 23; 1465498
Abstract (Summary)

As an active transporter of anionic molecules in the kidney, OAT3 plays a role in the renal elimination of many drugs and is also thought to be involved in drug-drug interactions in the kidney. A number of drugs have been identified as substrates or inhibitors of OAT3 including several non-steroidal anti-inflammatory drugs (NSAIDs) and various antibiotics. To date, most studies of drug interactions with OAT3 have focused on a few compounds or at most, a small panel of structural analogs. The goal of the current study was to identify FDA approved drugs that interact with OAT3 using a high-throughput screening approach. A library of 937 FDA approved drugs was screened using a cell-based fluorescence assay. A total of 55 drugs were identified as hits including NSAIDS, anti-diabetic agents, and macrolide antibiotics not previously known to interact with OAT3. Kinetics profiles were generated for a selection of drugs as validation for the screen.

Indexing (document details)
Advisor: Giacomini, Kathy M.
Commitee: Giacomini, Kathy M., Kroetz, Deanna L., Kwok, Pui Y.
School: University of California, San Francisco
Department: Pharmaceutical Sciences and Pharmacogenomics
School Location: United States -- California
Source: MAI 47/06M, Masters Abstracts International
Subjects: Pharmacology
Keywords: Drug drug interaction, Membrane transporters, OAT3, Screen
Publication Number: 1465498
ISBN: 978-1-109-20960-0
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