新型药物安非他尼与微管蛋白的相互作用。
Interaction of the novel agent amphethinile with tubulin.
作者信息
McGown A T, Fox B W
机构信息
Paterson Institute for Cancer Research, Christie Hospital and Holt Radium Institute, Manchester, UK.
出版信息
Br J Cancer. 1989 Jun;59(6):865-8. doi: 10.1038/bjc.1989.183.
Abstract
The novel agent amphethinile is shown to inhibit tubulin assembly in vitro. This agent is capable of displacing colchicine but not vinblastine from tubulin and causes a stimulation in GTPase activity in vitro. The affinity constant for the association of this drug with tubulin has been determined (Ka = 1.3 x 10(6) M-1). It is concluded that amphethinile belongs to the class of agents which share a common binding site with colchicine on the tubulin molecule.
摘要
新型药物安非他明在体外可抑制微管蛋白组装。该药物能够将秋水仙碱从微管蛋白上置换下来，但不能置换长春花碱，且在体外可刺激鸟苷三磷酸酶（GTPase）活性。已测定该药物与微管蛋白结合的亲和常数（Ka = 1.3 x 10(6) M-1）。得出的结论是，安非他明属于在微管蛋白分子上与秋水仙碱共用一个结合位点的药物类别。
相似文献
1
Interaction of the novel agent amphethinile with tubulin.新型药物安非他尼与微管蛋白的相互作用。
Br J Cancer. 1989 Jun;59(6):865-8. doi: 10.1038/bjc.1989.183.
2
Structural and biochemical comparison of the anti-mitotic agents colchicine, combretastatin A4 and amphethinile.抗有丝分裂剂秋水仙碱、康普瑞他汀A4和安非他尼的结构与生化比较
Anticancer Drug Des. 1989 Mar;3(4):249-54.
3
4
CXI-benzo-84 reversibly binds to tubulin at colchicine site and induces apoptosis in cancer cells.CXI-苯并-84 可逆地结合到秋水仙碱位点的微管蛋白上，并诱导癌细胞凋亡。
Biochem Pharmacol. 2013 Aug 1;86(3):378-91. doi: 10.1016/j.bcp.2013.05.024. Epub 2013 Jun 6.
5
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.5,6-二氢吲哚并[2,1-α]异喹啉衍生物对微管蛋白聚合的抑制作用
J Med Chem. 1997 Oct 24;40(22):3524-33. doi: 10.1021/jm970177c.
6
Tubulin aggregation and disaggregation: mediation by two distinct vinblastine-binding sites.微管蛋白的聚合与解聚：由两个不同的长春花碱结合位点介导
Proc Natl Acad Sci U S A. 1976 Jul;73(7):2375-8. doi: 10.1073/pnas.73.7.2375.
7
The effect of TN-16 on the alkylation of tubulin.TN-16对微管蛋白烷基化的影响。
Biochem Biophys Res Commun. 1985 May 31;129(1):200-5. doi: 10.1016/0006-291x(85)91422-6.
8
Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization.甲氧基取代的3-甲酰基-2-苯基吲哚抑制微管蛋白聚合。
J Med Chem. 1998 Dec 3;41(25):4965-72. doi: 10.1021/jm980228l.
9
Binding of colchicine to beef brain tubulin: influence of methodology on binding constants.秋水仙碱与牛脑微管蛋白的结合：方法学对结合常数的影响。
Methods Find Exp Clin Pharmacol. 1984 Nov;6(11):679-84.
10
Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain.通过改善微管蛋白与秋水仙碱结构域附近潜在结合位点的结合亲和力，发现具有纳摩尔效力抗肿瘤活性的 4β-NH-(6-氨基吲哚)-4-去氧鬼臼毒素。
Eur J Med Chem. 2019 May 15;170:73-86. doi: 10.1016/j.ejmech.2019.03.006. Epub 2019 Mar 8.
本文引用的文献
1
Nucleotide and corresponding amino acid sequences encoded by alpha and beta tubulin mRNAs.α和β微管蛋白mRNA编码的核苷酸及相应氨基酸序列。
Nature. 1981 Feb 19;289(5799):650-5. doi: 10.1038/289650a0.
2
The interaction of vincristine with calf brain tubulin.长春新碱与小牛脑微管蛋白的相互作用。
J Biol Chem. 1983 Feb 10;258(3):1689-97.
3
The effect of vinca alkaloids in enhancing the sensitivity of a methotrexate-resistant (L1210/R7A) line, studied by flow cytometric and chromosome number analysis.通过流式细胞术和染色体数分析研究长春花生物碱增强甲氨蝶呤耐药（L1210/R7A）细胞系敏感性的作用。
Cancer Chemother Pharmacol. 1984;13(1):47-53. doi: 10.1007/BF00401447.
4
Interactions of combretastatin, a new plant-derived antimitotic agent, with tubulin.一种新型植物源抗有丝分裂剂——柯里拉京与微管蛋白的相互作用。
Biochem Pharmacol. 1983 Dec 15;32(24):3864-7. doi: 10.1016/0006-2952(83)90163-6.
5
Interactions of a new antimitotic agent, NSC-181928, with purified tubulin.一种新型抗有丝分裂剂NSC-181928与纯化微管蛋白的相互作用。
Biochem Biophys Res Commun. 1982 Feb 11;104(3):929-36. doi: 10.1016/0006-291x(82)91338-9.
6
A rapid method for quantitative determination of microtubule protein using DEAE-cellulose filters.一种使用DEAE-纤维素滤膜定量测定微管蛋白的快速方法。
Anal Biochem. 1972 Dec;50(2):373-85. doi: 10.1016/0003-2697(72)90046-2.
7
Microtubule assembly in the absence of added nucleotides.在未添加核苷酸的情况下微管装配。
Proc Natl Acad Sci U S A. 1973 Mar;70(3):765-8. doi: 10.1073/pnas.70.3.765.
8
Microtubular protein impairment by pentanal and hexanal.戊醛和己醛对微管蛋白的损害
Cell Biochem Funct. 1987 Jul;5(3):189-94. doi: 10.1002/cbf.290050306.
9
10
Pre-clinical studies of a novel anti-mitotic agent, amphethinile.新型抗有丝分裂剂安非替尼的临床前研究。
Br J Cancer. 1988 Feb;57(2):157-9. doi: 10.1038/bjc.1988.32.
Zotero 插件