ABCB1 p.Asn508Ile
| Predicted by SNAP2: | A: D (66%), C: D (59%), D: D (63%), E: D (66%), F: D (71%), G: D (53%), H: N (66%), I: D (71%), K: D (66%), L: D (71%), M: D (66%), P: D (80%), Q: D (53%), R: D (71%), S: D (59%), T: D (59%), V: D (71%), W: D (75%), Y: D (53%), |
| 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, P: D, Q: D, R: D, S: D, T: D, V: D, W: D, Y: D, |
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[hide] Biological effect of tyrosine kinase inhibitors on... J Vet Pharmacol Ther. 2011 Apr 12. doi: 10.1111/j.1365-2885.2011.01296.x. Takeuchi Y, Fujino Y, Fukushima K, Watanabe M, Nakagawa T, Ohno K, Sasaki N, Sugano S, Tsujimoto H
Biological effect of tyrosine kinase inhibitors on three canine mast cell tumor cell lines with various KIT statuses.
J Vet Pharmacol Ther. 2011 Apr 12. doi: 10.1111/j.1365-2885.2011.01296.x., 2011-04-12 [PMID:21480930]
Abstract [show]
Takeuchi, Y., Fujino, Y., Fukushima, K., Watanabe, M., Nakagawa, T., Ohno, K., Sasaki, N., Sugano, S., Tsujimoto, H. Biological effect of tyrosine kinase inhibitors on three canine mast cell tumor cell lines with various KIT statuses. J. vet. Pharmacol. Therap. doi: 10.1111/j.1365-2885.2011.01296.x. Tyrosine kinase inhibitors (TKIs) can be important in the treatment of canine mast cell tumor (cMCT). Meanwhile, some TKIs have been identified as substrates for ABCB1. The inhibitory effect of four TKIs (axitinib, imatinib, masitinib, and vatalanib) for proliferation and phosphorylation of c-Kit receptor as well as the expression and function of ABCB1 were investigated in three cMCT cell lines (HRMC, VIMC1, and CMMC1). The IC(50) values of the TKIs in HRMC, the only cell line with wild-type KIT, were clearly higher than those in CMMC1 and VIMC1. In HRMC and CMMC1, both the growth and phosphorylation of c-Kit receptor were suppressed proportionally by the TKIs. VIMC1 required higher concentrations for the inhibition of c-Kit receptor phosphorylation than those in cell growth. The treatment with cyclosporine increased the effects of the TKIs on VIMC1 since ABCB1 was expressed in VIMC1. The results indicated that cMCT cell lines harboring wild-type KIT had lower sensitivity to TKIs. The growth of VIMC1 was seemingly reduced by TKIs through the inhibition of other tyrosine kinases than c-Kit receptor. There was little influence of ABCB1 on TKI effects to the proliferation of VIMC1. These results will be helpful to understand the different sensitivity to TKIs in cMCT patients.
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No. Sentence Comment
60 These data are cited from our previous study (Takeuchi et al., 2010) Cell lines KIT mutation* Amino acid change Mutated exon Mutated domain HRMC - - - - CMMC1 Variant A 763-765 Del CAG 255 Del Gln Exon 5 Extracellular Variant B 1243 (A fi G) Lys415 Glu Exon 8 Extracellular ITD1718-1771 ITD573-590 Exon 11 Juxtamembrane Variant C 1521-1522 Ins T Nonsense mutation Exon 9 Extracellular VIMC1 1523 (A fi T) Asn508 Ile Exon 9 Extracellular ITD, internal tandem duplication.
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ABCB1 p.Asn508Ile 21480930:60:405
status: NEW