Pub. Date : 2017 Jan 15
PMID : 27816545
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. | abemaciclib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | Here, we found that LY2835219 remarkably enhanced the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 over-expressing cancer cells in vitro and in vivo. | abemaciclib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | Furthermore, LY2835219 significantly increased the intracellular accumulation of doxorubicin (DOX) and rhodamine 123 (Rho 123) by inhibiting ABCB1 or ABCG2-mediated drug efflux in the transporters-overexpressing cells. | abemaciclib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | Mechanistically, LY2835219 is likely a competitive inhibitor of ABCB1 and ABCG2 for its competition with [125I]-iodoarylazidoprazosin for photo affinity labeling of the transporters. | abemaciclib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | In conclusion, these findings revealed a novel role of LY2835219 in reversing ABCB1 or ABCG2-mediated MDR, which may be benefit to the patients with MDR cancer for combinational therapy. | abemaciclib | ATP binding cassette subfamily B member 1 | Homo sapiens |