Paclitaxel Hydrogelator Delays Microtubule Aggregation |
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Authors: | Bin Mei Gao-lin Liang |
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Institution: | 1.CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, Hefei 230026, China;Department of Biology, College of Life Science, Anhui Medical University, Hefei 230032, China2.CAS Key Laboratory of Soft Matter Chemistry, Department of Chemistry, University of Science and Technology of China, Hefei 230026, China |
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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. |
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Keywords: | Paclitaxel Hydrogelator Microtubule Aggregation |
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