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Paclitaxel Hydrogelator Delays Microtubule Aggregation
中国科技大学化学系
Author NameAffiliationE-mail
中国科技大学化学系 中国科技大学化学系 gliang@ustc.edu.cn 
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 hydrogelator Fmoc-Phe-Phe-Lys(PTX)-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 1 obviously delayed microtubule aggregation than PTX did. Under the catalysis of alkaline phosphatase, 1 could self-assemble into nanofiber Fmoc-Phe-Phe-Lys(PTX)-Tyr-OH (2) with width comparable to the size of ??-tubulin dimer. Therefore, we proposed in this work that nanofiber 2 not only inhibits the ??-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
FundProject:
Paclitaxel Hydrogelator Delays Microtubule Aggregation
梁高林
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(PTX)-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 1 obviously delayed microtubule aggregation than PTX did. Under the catalysis of alkaline phosphatase, 1 could self-assemble into nanofiber Fmoc-Phe-Phe-Lys(PTX)-Tyr-OH (2) with width comparable to the size of ??-tubulin dimer. Therefore, we proposed in this work that nanofiber 2 not only inhibits the ??-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
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