A high throughput flow cytometric assay platform targeting transporter inhibition

Area of Science:

• Biochemistry
• Molecular Biology
• Pharmacology

Background:

• Efflux pumps are crucial in drug resistance and cellular transport.
• High Throughput Screening (HTS) offers efficient methods for drug discovery.
• Flow cytometry provides a versatile platform for cellular analysis.

Purpose of the Study:

• To review the concepts, applications, and limitations of HTS flow cytometry-based efflux inhibitory assays.
• To highlight the potential of this platform in identifying novel transporter inhibitors.
• To explore its utility in targeting microbial efflux systems.

Main Methods:

• Utilizing flow cytometry for HTS of efflux inhibitory assays.
• Employing mammalian and yeast efflux systems for assay development.
• Analyzing data for identification of small molecules with transporter inhibitory capabilities.

Main Results:

• Successful application in mammalian and yeast efflux systems.
• Identification of small molecules with transporter inhibitory capabilities.
• Demonstration of substrate multiplexing potential.

Conclusions:

• HTS flow cytometry-based efflux assays are effective for identifying transporter inhibitors.
• This platform can facilitate novel strategies against microbial efflux systems.
• The generated datasets can map the chemistry-transporter biology interface in pathogenic systems.