Abstract
Alpha-momorcharin (α-MMC) is a ribosome-inactivating protein (RIP) with excellent cytotoxicity to tumor cells. However, its strong immunogenicity and short plasma half-life limit its clinical applications. To overcome this, we have to PEGylated α-MMC using a branched 20 kDa (mPEG) 2-Lys-NHS. Homogeneous mono-, di- and tri-PEGylated α-MMCs were synthesized, purified and characterized. In vitro and in vivo analysis indicated that the serial PEG-conjugates preserved moderate anti-tumor activity with 36% acute toxicity and at most 66% immunogenicity decrease. These results suggested the potential application of α-MMC-PEG conjugates as an anti-tumor agent.
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This work was supported by the National Science Foundation of China (Grant No. 30770232).
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Bian, X., Shen, F., Chen, Y. et al. PEGylation of alpha-momorcharin: synthesis and characterization of novel anti-tumor conjugates with therapeutic potential. Biotechnol Lett 32, 883–890 (2010). https://doi.org/10.1007/s10529-010-0242-8
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DOI: https://doi.org/10.1007/s10529-010-0242-8