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紫杉醇水凝胶成胶因子延缓微管蛋白聚集
梅斌,梁高林*
作者单位E-mail
梅斌 中国科学技术大学化学系, 中科院软物质化学重点实验室, 合肥 230026;安徽医科大学生命科学学院生物系, 合肥 230032  
梁高林* 中国科学技术大学化学系, 中科院软物质化学重点实验室, 合肥 230026 gliang@ustc.edu.cn 
摘要:
关键词:  
DOI:10.1063/1674-0068/30/cjcp1609179
分类号:
基金项目:This work was supported by the Ministry of Sci-ence and Technology of China (No.2016YFA0400904) and the National Natural Science Foundation of China (No.U1532144 and No.21675145)
Paclitaxel Hydrogelator Delays Microtubule Aggregation
Bin Mei,Gao-lin Liang*
Abstract:
Paclitaxel (PTX) is one of the most efficient anticancer drugs for the treatment of cancers through β-tubulin-binding. Our previous work indicated that a PTX-derivative hydroge-lator Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr(H2PO3)-OH (1)could promote neuron branching but the underlying mechanism remains unclear. Using tubulin assembly-disassembly assay, in this work, we found that compound 1 obviously delayed more microtubule aggregation than PTX did. Under the catalysis of alkaline phosphatase, Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr(H2PO3)-OH could self-assemble into nanofiber Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr-OH with width comparable to the size of αβ-tubulin dimer. Therefore, we proposed in this work that nanofiber Fmoc-Phe-Phe-Lys(paclitaxel)-Tyr-OH not only inhibits the αβ-tubulin dimer binding to each other but also interferes with the plus end aggregation of microtubule. This work provides a new mechanism of the inhibition of microtubule formation by a PTX-derivative hydrogelator.
Key words:  Paclitaxel  Hydrogelator  Microtubule  Aggregation