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Proc Natl Acad Sci U S A. 2004 Jul 6;101(27):10006-11. doi: 10.1073/pnas.0403459101. Epub 2004 Jun 28.
2
Rotational-echo double-resonance NMR distance measurements for the tubulin-bound Paclitaxel conformation.用于微管蛋白结合紫杉醇构象的旋转回波双共振核磁共振距离测量。
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3
Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.微管蛋白结合紫杉醇构象的评估：C-4至C-3'桥连紫杉醇类似物的合成、生物学及构效关系研究
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The tubulin-bound conformation of paclitaxel: T-taxol vs "PTX-NY".紫杉醇与微管蛋白结合的构象：T-紫杉醇与“PTX-NY”。
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7
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The T-Taxol conformation.T-紫杉醇构象
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The binding conformation of Taxol in beta-tubulin: a model based on electron crystallographic density.紫杉醇在β-微管蛋白中的结合构象：基于电子晶体学密度的模型
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Synthesis and bioactivity of a side chain bridged paclitaxel: A test of the T-Taxol conformation.一种侧链桥连紫杉醇的合成与生物活性：T-紫杉醇构象的检验
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Drugs That Changed Society: Microtubule-Targeting Agents Belonging to Taxanoids, Macrolides and Non-Ribosomal Peptides.改变社会的药物：属于紫杉烷类、大环内酯类和非核糖体肽的微管靶向药物。
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Alcyonacea: A Potential Source for Production of Nitrogen-Containing Metabolites.海柳珊瑚：含氮代谢产物的潜在来源。
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Quest for Efficacious Next-Generation Taxoid Anticancer Agents and Their Tumor-Targeted Delivery.探寻高效的下一代紫杉烷类抗癌药物及其肿瘤靶向递送。
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Conformationally Constrained and Nanoparticle Targeted Paclitaxels.构象受限且靶向纳米颗粒的紫杉醇
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10
Drug discovery targeting cell division proteins, microtubules and FtsZ.针对细胞分裂蛋白、微管和FtsZ的药物研发
Bioorg Med Chem. 2014 Sep 15;22(18):5060-77. doi: 10.1016/j.bmc.2014.02.036. Epub 2014 Mar 5.

本文引用的文献

1
Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain.从与秋水仙碱和类微管相关蛋白结构域的复合物中洞察微管蛋白调控机制。
Nature. 2004 Mar 11;428(6979):198-202. doi: 10.1038/nature02393.
2
Modeling the interaction of paclitaxel with beta-tubulin.模拟紫杉醇与β-微管蛋白的相互作用。
Oncol Res. 2003;14(1):1-19. doi: 10.3727/000000003108748568.
3
Synthesis of novel C2-C3'N-linked macrocyclic taxoids by means of highly regioselective Heck macrocyclization.
Org Lett. 2003 Oct 2;5(20):3733-6. doi: 10.1021/ol0354627.
4
Synthesis of novel macrocyclic docetaxel analogues. Influence of their macrocyclic ring size on tubulin activity.新型大环多西他赛类似物的合成。其大环环大小对微管蛋白活性的影响。
J Med Chem. 2003 Aug 14;46(17):3623-30. doi: 10.1021/jm030770w.
5
Microtubule structure at 8 A resolution.8埃分辨率下的微管结构。
Structure. 2002 Oct;10(10):1317-28. doi: 10.1016/s0969-2126(02)00827-4.
6
Anticancer therapy with novel tubulin-interacting drugs.使用新型微管蛋白相互作用药物的抗癌治疗。
Drug Resist Updat. 2001 Dec;4(6):392-401. doi: 10.1054/drup.2002.0230.
7
Refined structure of alpha beta-tubulin at 3.5 A resolution.分辨率为3.5埃的αβ-微管蛋白精细结构。
J Mol Biol. 2001 Nov 9;313(5):1045-57. doi: 10.1006/jmbi.2001.5077.
8
The interaction of baccatin III with the taxol binding site of microtubules determined by a homogeneous assay with fluorescent taxoid.通过荧光紫杉烷类化合物的均相测定法确定巴卡亭III与微管蛋白紫杉醇结合位点的相互作用。
Biochemistry. 2001 Oct 9;40(40):11975-84. doi: 10.1021/bi010869+.
9
Synthesis and biological evaluation of novel macrocyclic paclitaxel analogues.新型大环紫杉醇类似物的合成与生物学评价
Org Lett. 2001 Aug 9;3(16):2461-4. doi: 10.1021/ol016124d.
10
Novel d-seco paclitaxel analogues: synthesis, biological evaluation, and model testing.新型二去甲紫杉醇类似物：合成、生物学评价及模型测试。
J Org Chem. 2001 May 18;66(10):3321-9. doi: 10.1021/jo0015467.

β-微管蛋白上的生物活性紫杉醇构象：来自高活性受限类似物的实验证据。

The bioactive Taxol conformation on beta-tubulin: experimental evidence from highly active constrained analogs.

作者信息

Ganesh Thota, Guza Rebecca C, Bane Susan, Ravindra Rudravajhala, Shanker Natasha, Lakdawala Ami S, Snyder James P, Kingston David G I

机构信息

Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.

出版信息

Proc Natl Acad Sci U S A. 2004 Jul 6;101(27):10006-11. doi: 10.1073/pnas.0403459101. Epub 2004 Jun 28.

DOI:10.1073/pnas.0403459101
PMID:15226503
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC454156/
Abstract

The important anticancer drug Taxol (paclitaxel) binds to tubulin in a stoichiometric ratio and promotes its assembly into microtubules. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been made. In this work we present experimental and theoretical evidence that Taxol adopts a T-shaped conformation when it is bound to tubulin.

摘要

重要的抗癌药物紫杉醇（paclitaxel）以化学计量比与微管蛋白结合，并促进其组装成微管。与微管结合的药物的构象一直是深入研究的主题，并且已经提出了各种建议。在这项工作中，我们提供了实验和理论证据，表明紫杉醇与微管蛋白结合时呈T形构象。