文献类型：期刊文章

作　　者：梅斌[1,2] 梁高林[1]

机构地区：[1]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 [2]安徽医科大学生命科学学院生物系,合肥230032

出　　处：《Chinese Journal of Chemical Physics》

基　　金：This work was supported by the Ministry of Science and Technology of China （No.2016YFA0400904） and the National Natural Science Foundation of China （No.U1532144 and No.21675145）.

年　　份：2017

卷　　号：30

期　　号：2

起止页码：239-242

语　　种：中文

收录情况：0、AJ、CAS、CSCD、CSCD2017_2018、INSPEC、JST、RSC、SCI-EXPANDED(收录号：WOS:000400934100018)、SCIE、SCOPUS、WOS、ZGKJHX、普通刊

摘　　要：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 hydrogelator 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.

关 键 词：PACLITAXEL HYDROGELATOR MICROTUBULE AGGREGATION

分 类 号：O]