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BIOMARKER:

ABCG2 overexpression

i
Other names: ABCG2, ABCP, BCRP, CD338, EST157481, MXR, ATP-binding cassette, sub-family G (WHITE), member 2 (Junior blood group)
Entrez ID:
12d
In this study, we discovered that by attenuating the drug transport function of ABCG2, TP-3654 resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic ABCG2 substrate drugs topotecan, SN-38 and mitoxantrone. Moreover, our results indicate that ABCG2 does not mediate resistance to TP-3654 and may not play a major role in the induction of resistance to TP-3654 in cancer patients. Taken together, our findings reveal that TP-3654 is a selective, potent modulator of ABCG2 drug efflux function that may offer an additional combination therapy option for the treatment of multidrug-resistant cancers.
Journal
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ABCG2
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ABCG2 overexpression
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topotecan • mitoxantrone • TP-3654
2ms
In vitro, 3 μM of GS-9973 reversed the drug resistance of NCI-H460/MX20 cell line to mitoxantrone or doxorubicin. Finally, HPLC analysis proved that the intracellular concentration of GS-9973 is not significantly different in both parental and resistant cell lines. In conclusion, our study suggests that in vitro, GS-9973 in combination with certain anticancer drugs, represent a strategy to overcome ABCG2-mediated MDR cancers.
Journal
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ABCG2 • SYK (Spleen tyrosine kinase)
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ABCG2 overexpression
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doxorubicin hydrochloride • entospletinib (GS-9973) • mitoxantrone
2ms
More resistance to chemotherapeutics and altered gene expression profile was shown in 3D cell cultures when compared with the 2D cells. These results might play an important role to evaluate the efficacy of anticancer drugs, explore mechanisms of MDR in the 3D spheroid forms.
Preclinical • Journal
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ABCG2
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ABCG2 overexpression
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cisplatin • gemcitabine • 5-fluorouracil • irinotecan
4ms
Finally, VKNG-2 produced a significant concentration-dependent increase in ATPase activity (EC = 2.3 µM). In conclusion, our study suggests that in vitro, VKNG-2 reverses the resistance of S1-M1-80, a cancer cell line resistant to mitoxantrone and SN-38, by inhibiting the efflux function of the ABCG2 transporter.
Preclinical • Journal
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AKT1 (V-akt murine thymoma viral oncogene homolog 1) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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ABCG2 overexpression
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mitoxantrone
5ms
Moreover, this SMAR1/ABCG2 axis positively regulates the chemotherapeutic sensitivity of OS cells. This work indicates that SMAR1 is a critical suppressor for OS progression through transcriptionally regulating ABCG2 expression.
Journal
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ABCG2 • HDAC2 (Histone deacetylase 2)
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ABCG2 overexpression
7ms
A novel mRNA 3’UTR shortening machinery was shown to mediate the simultaneous overexpression of ABCG2 and CD133 in SP and CSC cells. It may represent useful drug target for circumvention of resistance and eradication of CSCs.
Late-breaking abstract
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ABCG2 • CD133 • BMI1 (BMI1 proto-oncogene, polycomb ring finger)
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ABCG2 overexpression • CD133 expression • CD133 overexpression