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In vivo evidence of complete circumvention of vincristine resistance by a new triazinoaminopiperidine derivative S 9788 in P388/VCR leukemia model.

作者信息

Cros S, Guilbaud N, Berlion M, Dunn T, Regnier G, Dhainaut A, Atassi G, Bizzari J P

机构信息

C.N.R.S., Laboratoire de Pharmacologie et Toxicologie Fondamentales, Toulouse, France.

出版信息

Cancer Chemother Pharmacol. 1992;30(6):491-4. doi: 10.1007/BF00685604.

DOI:10.1007/BF00685604
PMID:1394807
Abstract

S 9788, a new triazinoaminopiperidine derivative, was found to be a potent reversant of vincristine resistance in the in vivo murine leukemic P388/VCR model. In two treatment regimens (Q4D days 1, 5 and 9 and QD days 1-9), S 9788 enhanced the antitumor activity of vincristine in a dose-dependent manner, resulting in a complete circumvention of drug resistance for well-tolerated doses of S 9788. S 9788 was also effective in enhancing therapeutic effects of vincristine in the treatment of sensitive P388-bearing mice. These results strongly suggest that S 9788 may be a potential candidate for circumvention of multidrug resistance (MDR) in clinical practice.

摘要

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1
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2
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3
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本文引用的文献

1
Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil.通过维拉帕米增强长春新碱和长春碱的细胞毒性在体内和体外克服P388白血病对长春新碱的耐药性
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Cure of mice bearing P388 leukemia by vincristine in combination with a calcium channel blocker.
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Multiple-drug resistance in human cancer.人类癌症中的多药耐药性。
N Engl J Med. 1987 May 28;316(22):1388-93. doi: 10.1056/NEJM198705283162207.
阿霉素联合多药耐药逆转剂S9788治疗晚期结直肠癌和肾细胞癌的I B期研究
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4
Modulation of multidrug resistance by SDZ PSC 833 in leukemic and solid-tumor-bearing mouse models.在白血病和荷实体瘤小鼠模型中,SDZ PSC 833对多药耐药性的调节作用。
Jpn J Cancer Res. 1996 Feb;87(2):184-93. doi: 10.1111/j.1349-7006.1996.tb03157.x.
5
Multidrug resistance circumvention by a new triazinoaminopiperidine derivative S9788 in vitro: definition of the optimal schedule and comparison with verapamil.新型三嗪氨基哌啶衍生物S9788在体外克服多药耐药性:最佳给药方案的确定及与维拉帕米的比较
Br J Cancer. 1994 May;69(5):868-74. doi: 10.1038/bjc.1994.168.
6
In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients.S 9788对多药耐药白血病细胞系和正常造血细胞的体外活性——I期治疗患者血清逆转多药耐药性
Cancer Chemother Pharmacol. 1995;36(3):195-203. doi: 10.1007/BF00685846.
7
Binding of a new multidrug resistance modulator, S9788, to human plasma proteins and erythrocytes.
Invest New Drugs. 1995;13(1):37-41. doi: 10.1007/BF02614218.
4
Expression of a full-length cDNA for the human "MDR1" gene confers resistance to colchicine, doxorubicin, and vinblastine.人类“MDR1”基因全长cDNA的表达赋予了对秋水仙碱、阿霉素和长春花碱的抗性。
Proc Natl Acad Sci U S A. 1987 May;84(9):3004-8. doi: 10.1073/pnas.84.9.3004.
5
Effect of verapamil on doxorubicin activity and pharmacokinetics in mice bearing resistant and sensitive solid tumors.维拉帕米对荷耐药和敏感实体瘤小鼠阿霉素活性及药代动力学的影响。
Cancer Chemother Pharmacol. 1988;21(4):329-36. doi: 10.1007/BF00264200.
6
Physical-chemical properties shared by compounds that modulate multidrug resistance in human leukemic cells.调节人类白血病细胞多药耐药性的化合物共有的物理化学性质。
Mol Pharmacol. 1988 Apr;33(4):454-62.
7
Isolation and expression of a complementary DNA that confers multidrug resistance.一种赋予多药耐药性的互补DNA的分离与表达。
Nature. 1986;323(6090):728-31. doi: 10.1038/323728a0.
8
In vivo circumvention of vincristine resistance in mice with P388 leukemia using a novel compound, AHC-52.
Cancer Res. 1989 Apr 1;49(7):1722-6.
9
Mechanism of multidrug resistance.多药耐药机制。
Biochim Biophys Acta. 1988 Aug 3;948(1):87-128. doi: 10.1016/0304-419x(88)90006-6.
10
Essential features of the P-glycoprotein pharmacophore as defined by a series of reserpine analogs that modulate multidrug resistance.由一系列调节多药耐药性的利血平类似物所定义的P-糖蛋白药效基团的基本特征。
Proc Natl Acad Sci U S A. 1989 Jul;86(13):5128-32. doi: 10.1073/pnas.86.13.5128.