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由Peloruside A诱导的独特微管稳定模式。

A unique mode of microtubule stabilization induced by peloruside A.

作者信息

Huzil J Torin, Chik John K, Slysz Gordon W, Freedman Holly, Tuszynski Jack, Taylor Richard E, Sackett Dan L, Schriemer David C

机构信息

Division of Experimental Oncology, Cross Cancer Institute, 11560 University Avenue, Edmonton, Alberta, Canada.

出版信息

J Mol Biol. 2008 May 16;378(5):1016-30. doi: 10.1016/j.jmb.2008.03.026. Epub 2008 Mar 19.


DOI:10.1016/j.jmb.2008.03.026
PMID:18405918
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2441936/
Abstract

Microtubules are significant therapeutic targets for the treatment of cancer, where suppression of microtubule dynamicity by drugs such as paclitaxel forms the basis of clinical efficacy. Peloruside A, a macrolide isolated from New Zealand marine sponge Mycale hentscheli, is a microtubule-stabilizing agent that synergizes with taxoid drugs through a unique site and is an attractive lead compound in the development of combination therapies. We report here unique allosteric properties of microtubule stabilization via peloruside A and present a structural model of the peloruside-binding site. Using a strategy involving comparative hydrogen-deuterium exchange mass spectrometry of different microtubule-stabilizing agents, we suggest that taxoid-site ligands epothilone A and docetaxel stabilize microtubules primarily through improved longitudinal interactions centered on the interdimer interface, with no observable contributions from lateral interactions between protofilaments. The mode by which peloruside A achieves microtubule stabilization also involves the interdimer interface, but includes contributions from the alpha/beta-tubulin intradimer interface and protofilament contacts, both in the form of destabilizations. Using data-directed molecular docking simulations, we propose that peloruside A binds within a pocket on the exterior of beta-tubulin at a previously unknown ligand site, rather than on alpha-tubulin as suggested in earlier studies.

摘要

微管是癌症治疗的重要靶点,像紫杉醇这类药物抑制微管动态性构成了临床疗效的基础。Peloruside A是一种从新西兰海洋海绵Mycale hentscheli中分离出的大环内酯类化合物,是一种微管稳定剂,它通过一个独特的位点与紫杉烷类药物协同作用,是联合疗法开发中一种有吸引力的先导化合物。我们在此报告通过Peloruside A实现微管稳定的独特变构特性,并展示Peloruside结合位点的结构模型。通过一种涉及对不同微管稳定剂进行比较氢-氘交换质谱分析的策略,我们认为紫杉烷类位点配体埃坡霉素A和多西他赛主要通过改善以二聚体间界面为中心的纵向相互作用来稳定微管,原纤维之间的横向相互作用没有明显贡献。Peloruside A实现微管稳定的方式也涉及二聚体间界面,但包括来自α/β-微管蛋白二聚体内界面和原纤维接触的贡献,二者均以去稳定化的形式存在。利用数据导向的分子对接模拟,我们提出Peloruside A结合在β-微管蛋白外部一个此前未知的配体位点的口袋内,而不是像早期研究所暗示的那样结合在α-微管蛋白上。

相似文献

[1]
A unique mode of microtubule stabilization induced by peloruside A.

J Mol Biol. 2008-5-16

[2]
Hallmarks of molecular action of microtubule stabilizing agents: effects of epothilone B, ixabepilone, peloruside A, and laulimalide on microtubule conformation.

J Biol Chem. 2011-1-18

[3]
Structural basis of microtubule stabilization by laulimalide and peloruside A.

Angew Chem Int Ed Engl. 2014-1-27

[4]
Peloruside A does not bind to the taxoid site on beta-tubulin and retains its activity in multidrug-resistant cell lines.

Cancer Res. 2004-8-1

[5]
Peloruside A: a lead non-taxoid-site microtubule-stabilizing agent with potential activity against cancer, neurodegeneration, and autoimmune disease.

Nat Prod Rep. 2016-2-12

[6]
Distinct pose of discodermolide in taxol binding pocket drives a complementary mode of microtubule stabilization.

Biochemistry. 2009-12-15

[7]
Modulation of lateral and longitudinal interdimeric interactions in microtubule models by Laulimalide and Peloruside A association: A molecular modeling approach on the mechanism of microtubule stabilizing agents.

Chem Biol Drug Des. 2018-1-23

[8]
Structural insight into the role of Gln293Met mutation on the Peloruside A/Laulimalide association with αβ-tubulin from molecular dynamics simulations, binding free energy calculations and weak interactions analysis.

J Comput Aided Mol Des. 2017-7

[9]
Peloruside A synergizes with other microtubule stabilizing agents in cultured cancer cell lines.

Mol Pharm. 2007

[10]
Molecular recognition of peloruside A by microtubules. The C24 primary alcohol is essential for biological activity.

Chembiochem. 2010-8-16

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[2]
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Sci Rep. 2024-12-4

[3]
Utilization of Photoaffinity Labeling to Investigate Binding of Microtubule Stabilizing Agents to P-Glycoprotein and β-Tubulin.

J Nat Prod. 2022-3-25

[4]
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Plant Mol Biol. 2021-3

[5]
Further Insight into the Interactions of the Cytotoxic Macrolides Laulimalide and Peloruside A with Their Common Binding Site.

ACS Omega. 2018-2-9

[6]
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.

J Nat Prod. 2017-2-24

[7]
2-(m-Azidobenzoyl)taxol binds differentially to distinct β-tubulin isotypes.

Proc Natl Acad Sci U S A. 2016-10-4

[8]
Biological Characterization of an Improved Pyrrole-Based Colchicine Site Agent Identified through Structure-Based Design.

Mol Pharmacol. 2016-2

[9]
Localizing Carbohydrate Binding Sites in Proteins Using Hydrogen/Deuterium Exchange Mass Spectrometry.

J Am Soc Mass Spectrom. 2016-1

[10]
Peloruside A is a microtubule-stabilizing agent with exceptional anti-migratory properties in human endothelial cells.

Oncoscience. 2015-6-12

本文引用的文献

[1]
Peloruside A synergizes with other microtubule stabilizing agents in cultured cancer cell lines.

Mol Pharm. 2007

[2]
Structural basis of the activity of the microtubule-stabilizing agent epothilone a studied by NMR spectroscopy in solution.

Angew Chem Int Ed Engl. 2007

[3]
Synergistic effects of peloruside A and laulimalide with taxoid site drugs, but not with each other, on tubulin assembly.

Mol Pharmacol. 2006-11

[4]
Hydrogen/deuterium-exchange (H/D-Ex) of PPARgamma LBD in the presence of various modulators.

Protein Sci. 2006-8

[5]
NMR determination of the bioactive conformation of peloruside A bound to microtubules.

J Am Chem Soc. 2006-7-12

[6]
The betaI/betaIII-tubulin isoforms and their complexes with antimitotic agents. Docking and molecular dynamics studies.

FEBS J. 2006-7

[7]
Insights into the mechanism of microtubule stabilization by Taxol.

Proc Natl Acad Sci U S A. 2006-7-5

[8]
Structural mechanisms underlying nucleotide-dependent self-assembly of tubulin and its relatives.

Curr Opin Struct Biol. 2006-4

[9]
Microtubule stabilizing agents: their molecular signaling consequences and the potential for enhancement by drug combination.

Cancer Treat Rev. 2006-5

[10]
Probing protein ligand interactions by automated hydrogen/deuterium exchange mass spectrometry.

Anal Chem. 2006-2-15

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