Identification of the side population associated with ATP-binding cassette transporters activity using imaging flow cytometry

2021 ◽  
Vol 67 (2) ◽  
pp. 137-143
Author(s):  
A.M. Gisina ◽  
Y.S. Kim ◽  
K.N. Yarygin ◽  
A.Yu. Lupatov
Keyword(s):  
Flow Cytometry ◽  
Side Population ◽  
Flow Cytometer ◽  
Atp Binding ◽  
Tumor Resistance ◽  
Side Population Cells ◽  
Imaging Flow Cytometry ◽  
Atp Binding Cassette Transporters ◽  
Resistance To Chemotherapy ◽  
Atp Binding Cassette

DyeCycle Violet efflux, caused by ATP-binding cassette transporters activity, was analyzed in human colorectal adenocarcinoma cell lines SW480, HT-29, Caco-2 by neans of FACSAria III flow cytometer and ImageStreamX Mk II imaging flow cytometer. Along with similarity of cytometry data obtained on the two instruments, the use of imaging flow cytometry made it possible to characterize the morphology of side population cells, as well as morphology of other cell populations differing in the degree of dye accumulation. The population of cells, which are smaller than the side population cells and practically do not take the dye, is of the special interest. Probably, this population may contribute to the tumor resistance to chemotherapy.

scholarly journals Role of the ATP-Binding Cassette TransporterAbcg2in the Phenotype and Function of Cardiac Side Population Cells

2008 ◽  
Vol 103 (8) ◽  
pp. 825-835 ◽  
Author(s):  
Otmar Pfister ◽  
Angelos Oikonomopoulos ◽  
Konstantina-Ioanna Sereti ◽  
Regina L. Sohn ◽  
Darragh Cullen ◽  
...  
Keyword(s):  
Side Population ◽  
Atp Binding ◽  
Side Population Cells ◽  
And Function ◽  
Atp Binding Cassette

scholarly journals Human limbal epithelium contains side population cells expressing the ATP-binding cassette transporter ABCG2

FEBS Letters ◽  
2004 ◽  
Vol 565 (1-3) ◽  
pp. 6-10 ◽  
Author(s):  
Katsuhiko Watanabe ◽  
Kohji Nishida ◽  
Masayuki Yamato ◽  
Terumasa Umemoto ◽  
Taizo Sumide ◽  
...  
Keyword(s):  
Side Population ◽  
Atp Binding ◽  
Side Population Cells ◽  
Atp Binding Cassette Transporter ◽  
Limbal Epithelium ◽  
Atp Binding Cassette

scholarly journals Stimulation of Cholesterol Excretion by the Liver X Receptor Agonist Requires ATP-binding Cassette Transporters G5 and G8

2003 ◽  
Vol 278 (18) ◽  
pp. 15565-15570 ◽  
Author(s):  
Liqing Yu ◽  
Jennifer York ◽  
Klaus von Bergmann ◽  
Dieter Lutjohann ◽  
Jonathan C. Cohen ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Liver X Receptor ◽  
Atp Binding ◽  
Atp Binding Cassette Transporters ◽  
Cholesterol Excretion ◽  
Liver X Receptor Agonist ◽  
Stimulation Of ◽  
Atp Binding Cassette

scholarly journals A Selective ATP-Binding Cassette Subfamily G Member 2 Efflux Inhibitor Revealed via High-Throughput Flow Cytometry

2012 ◽  
Vol 18 (1) ◽  
pp. 26-38 ◽  
Author(s):  
J. Jacob Strouse ◽  
Irena Ivnitski-Steele ◽  
Hadya M. Khawaja ◽  
Dominique Perez ◽  
Jerec Ricci ◽  
...  
Keyword(s):  
Molecular Probes ◽  
Atp Binding ◽  
Specific Substrate ◽  
Tumor Resistance ◽  
Drug Concentrations ◽  
Efflux Inhibition ◽  
Substrate Inhibitor ◽  
Atp Binding Cassette

Chemotherapeutics tumor resistance is a principal reason for treatment failure, and clinical and experimental data indicate that multidrug transporters such as ATP-binding cassette (ABC) B1 and ABCG2 play a leading role by preventing cytotoxic intracellular drug concentrations. Functional efflux inhibition of existing chemotherapeutics by these pumps continues to present a promising approach for treatment. A contributing factor to the failure of existing inhibitors in clinical applications is limited understanding of specific substrate/inhibitor/pump interactions. We have identified selective efflux inhibitors by profiling multiple ABC transporters against a library of small molecules to find molecular probes to further explore such interactions. In our primary screening protocol using JC-1 as a dual-pump fluorescent reporter substrate, we identified a piperazine-substituted pyrazolo[1,5-a]pyrimidine substructure with promise for selective efflux inhibition. As a result of a focused structure-activity relationship (SAR)–driven chemistry effort, we describe compound 1 (CID44640177), an efflux inhibitor with selectivity toward ABCG2 over ABCB1. Compound 1 is also shown to potentiate the activity of mitoxantrone in vitro as well as preliminarily in vivo in an ABCG2-overexpressing tumor model. At least two analogues significantly reduce tumor size in combination with the chemotherapeutic topotecan. To our knowledge, low nanomolar chemoreversal activity coupled with direct evidence of efflux inhibition for ABCG2 is unprecedented.

scholarly journals Endocrine Disruptors Differentially Target ATP-Binding Cassette Transporters in the Blood-Testis Barrier and Affect Leydig Cell Testosterone Secretion In Vitro

2013 ◽  
Vol 136 (2) ◽  
pp. 382-391 ◽  
Author(s):  
Anita C. A. Dankers ◽  
Maarke J. E. Roelofs ◽  
Aldert H. Piersma ◽  
Fred C. G. J. Sweep ◽  
Frans G. M. Russel ◽  
...  
Keyword(s):  
Endocrine Disruptors ◽  
Leydig Cell ◽  
Atp Binding ◽  
Testosterone Secretion ◽  
Atp Binding Cassette Transporters ◽  
Blood Testis Barrier ◽  
Atp Binding Cassette
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