Journal: Pharmaceutics
Article Title: Impact of V9302, a Competitive Antagonist of Transmembrane Glutamine Flux on Reversal of Resistance in Breast Cancer Cell Lines
doi: 10.3390/pharmaceutics16070877
Figure Lengend Snippet: ( A ): Rhodamine 123 accumulation in Pgp-overexpressing mouse T-lymphoma cells in the presence of V9302 at 2, 10, and 20 µM ( A ). Tariquidar was used at 0.2 µM as a positive control. PAR cells represent 100% rhodamine 123 accumulation. ( B ): Pgp ATPase inhibition: V9302 was applied at 20 µM. ∆RLU TC > ∆RLU basal : the tested compound (TC) is stimulator of Pgp ATPase activity; ∆RLU TC = ∆RLUbasal: the tested compound has no effect on Pgp ATPase activity; ∆RLU TC < ∆RLU basal : the tested compound is an inhibitor of Pgp ATPase activity, black line represents the basal Pgp ATPase activity, **** indicates p < 0.0001.
Article Snippet: The effect of V9302 ((2S)-2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]butanoic acid; MedChemExpress, Monmouth Junction, NJ, USA) ( ) was investigated on several cell lines: breast cancer cell line MCF-7 (ATCC ® HTB-22) (purchased from LGC Promochem (Teddington, Middlesex, UK)), and its doxorubicin-resistant subline KCR; HTB-26TM breast adenocarcinoma (ATCC ® MDA-MB-231); and T-47D (ATCC ® HTB-133TM) ductal carcinoma of the breast; L5178Y mouse T-lymphoma cells (ECACC catalog no. 87111908, US FDA, Silver Spring, MD, USA) were transfected with the pHa MDR1/A retrovirus, as previously reported [ ].
Techniques: Positive Control, Inhibition, Activity Assay