Pub. Date : 2020 Oct
PMID : 32634436
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Overexpression of ABCB1 and ABCG2 contributes to reduced efficacy of the PI3K/mTOR inhibitor samotolisib (LY3023414) in cancer cell lines. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | Overexpression of ABCB1 and ABCG2 contributes to reduced efficacy of the PI3K/mTOR inhibitor samotolisib (LY3023414) in cancer cell lines. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | In this study, we investigated whether the overexpression of ATP-binding cassette (ABC) drug transporters such as ABCB1 and ABCG2, one of the most common mechanisms for developing multidrug resistance, may potentially reduce the efficacy of LY3023414 in human cancer cells. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | We demonstrated that the intracellular accumulation of LY3023414 in cancer cells was significantly reduced by the drug efflux function of ABCB1 and ABCG2. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | Consequently, the cytotoxicity and efficacy of LY3023414 for inhibiting the activation of the PI3K pathway and induction of G0/G1 cell-cycle arrest were substantially reduced in cancer cells overexpressing ABCB1 or ABCG2, which could be restored using tariquidar or Ko143, respectively. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 6 | In conclusion, we report that LY3023414 is a substrate for ABCB1 and ABCG2 transporters implicating their role in the development of resistance to LY3023414, which can have substantial clinical implications and should be further investigated. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 7 | In conclusion, we report that LY3023414 is a substrate for ABCB1 and ABCG2 transporters implicating their role in the development of resistance to LY3023414, which can have substantial clinical implications and should be further investigated. | LY3023414 | ATP binding cassette subfamily B member 1 | Homo sapiens |