ABCC1 p.Thr24Ser
| Predicted by SNAP2: | A: D (63%), C: D (71%), D: D (85%), E: D (85%), F: D (85%), G: D (66%), H: D (85%), I: D (85%), K: D (85%), L: D (85%), M: D (85%), N: D (75%), P: D (59%), Q: D (75%), R: D (63%), S: N (61%), V: D (66%), W: D (91%), Y: D (85%), |
| Predicted by PROVEAN: | A: D, C: D, D: D, E: D, F: D, G: D, H: D, I: D, K: D, L: D, M: D, N: D, P: D, Q: D, R: D, S: N, V: D, W: D, Y: D, |
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[hide] Vinflunine (20',20'-difluoro-3',4'-dihydrovinorelb... Invest New Drugs. 1998;16(1):3-17. Etievant C, Barret JM, Kruczynski A, Perrin D, Hill BT
Vinflunine (20',20'-difluoro-3',4'-dihydrovinorelbine), a novel Vinca alkaloid, which participates in P-glycoprotein (Pgp)-mediated multidrug resistance in vivo and in vitro.
Invest New Drugs. 1998;16(1):3-17., [PMID:9740539]
Abstract [show]
Vinflunine (VFL) is a novel derivative of vinorelbine (NVB, Navelbine), which has shown markedly superior antitumor activity to NVB, in various experimental animal models. To establish whether this new Vinca alkaloid participates in P-glycoprotein (Pgp)-mediated multidrug resistance (MDR), VFL-resistant murine P388 cells (P388/VFL) were established in vivo and used in conjunction with the well established MDR P388/ADR subline, to define the in vivo resistance profile for VFL. P388/VFL cells proved cross-resistant to drugs implicated in MDR (other Vinca alkaloids, doxorubicin, etoposide), but not to campothecin or cisplatin and showed an increased expression of Pgp, without any detectable alterations in topoisomerase II or in glutathione metabolism. The P388/ADR cells proved cross-resistant to VFL both in vivo and in vitro, and this VFL resistance was efficiently modulated by verapamil in vitro. Cellular transport experiments with tritiated-VFL revealed differential uptake by P388 sensitive and P388/ADR resistant cells, comparable with data obtained using tritiated-NVB. In various in vitro models of human MDR tumor cells, whilst full sensitivity was retained in cells expressing alternative non-Pgp-mediated MDR mechanisms, cross resistance was identified in Pgp-overexpressing cells. Differences were, however, noted in terms of the drug resistance profiles relative to the other Vinca, with tumor cell lines proving generally least cross-resistant to VFL. Overall, these results suggest that VFL, like other Vinca alkaloids, participates in Pgp-mediated MDR, with tumor cells selected for resistance to VFL overexpressing Pgp, yet MDR tumor cell lines proved generally less cross resistant to VFL relative to the other Vinca alkaloids.
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No. Sentence Comment
79 The T24 sensitive (T24S) parental and the resistant T24M subline [28] were obtained from Dr R. Kiss, Laboratory of Histology, Université Libre de Bel- gique, ULB (Brussels, Belgium).
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ABCC1 p.Thr24Ser 9740539:79:19
status: NEW87 Cell culture conditions Parental and resistant human tumor cell lines were cultured in RPMI 1640 medium (Seromed, Poly- labo, Strasbourg, France) supplemented with 10% heat inactivated fetal calf serum (FCS, GIBCO, Cergy-Pontoise, France), except for T24S and T24M cells which were grown in MEM medium (GIBCO) supplemented with 5% FCS.
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ABCC1 p.Thr24Ser 9740539:87:251
status: NEW