A high throughput flow cytometric assay platform targeting transporter inhibition

Drug Discov Today Technol. 2014 Jun:12:e95-103. doi: 10.1016/j.ddtec.2014.03.010.

Abstract

This review highlights the concepts, recent applications and limitations of High Throughput Screening (HTS) flow cytometry-based efflux inhibitory assays. This platform has been employed in mammalian and yeast efflux systems leading to the identification of small molecules with transporter inhibitory capabilities. This technology offers the possibility of substrate multiplexing and may promote novel strategies targeting microbial efflux systems. This platform can generate a comprehensive dataset that may support efforts to map the interface between chemistry and transporter biology in a variety of pathogenic systems.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / antagonists & inhibitors*
  • Animals
  • Biological Transport
  • Drug Discovery / methods*
  • Flow Cytometry*
  • High-Throughput Screening Assays*
  • Humans
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Substrate Specificity

Substances

  • ATP-Binding Cassette Transporters
  • Small Molecule Libraries