title: A high throughput flow cytometric assay platform targeting transporter inhibition.
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.
authors.affiliation: Department of Dermatology, Harvard Medical School, Boston, MA 02114, United States.
authors.forename: George P
authors.initials: GP
authors.lastname: Tegos
authors.affiliation: Center for Molecular Discovery, University of New Mexico, Albuquerque, NM 87131, United States.
authors.forename: Annette M
authors.initials: AM
authors.lastname: Evangelisti
authors.affiliation: Center for Molecular Discovery, University of New Mexico, Albuquerque, NM 87131, United States.
authors.forename: J Jacob
authors.initials: JJ
authors.lastname: Strouse
authors.affiliation: Division of Translational Informatics, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, United States.
authors.forename: Oleg
authors.initials: O
authors.lastname: Ursu
authors.affiliation: Division of Translational Informatics, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, United States.
authors.forename: Cristian
authors.initials: C
authors.lastname: Bologa
authors.affiliation: Department of Pathology, University of New Mexico, School of Medicine, Albuquerque, NM 87131, United States.
authors.forename: Larry A
authors.initials: LA
authors.lastname: Sklar
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000037:antagonists & inhibitors*; D000818:Animals; D001692:Biological Transport; D055808:Drug Discovery / Q000379:methods*; D005434:Flow Cytometry; D057166:High-Throughput Screening Assays; D006801:Humans; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology*; D013379:Substrate Specificity
chemical_list: D018528:ATP-Binding Cassette Transporters; D054852:Small Molecule Libraries