High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3.

ABSTRACT:

Introduction

The organic cation transporter 3 (OCT3, SLC22A3) is ubiquitously expressed and interacts with a wide array of compounds including endogenous molecules, environmental toxins and prescription drugs. Understudied as a determinant of pharmacokinetics and pharmacodynamics, OCT3 has the potential to be a major determinant of drug absorption and disposition and to be a target for drug-drug interactions (DDIs).

Goal

The goal of the current study was to identify prescription drug inhibitors of OCT3.

Methods

We screened a compound library consisting of 2556 prescription drugs, bioactive molecules, and natural products using a high throughput assay in HEK-293 cells stably expressing OCT3.

Results

We identified 210 compounds that at 20 μM inhibit 50% or more o

SUBMITTER: Chen EC 

PROVIDER: S-EPMC9246766 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature