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- W3141472415 abstract "AIM: To assess the merits of polyethylene glycol-modified recombinant human tumor necrosis factor alpha (PEG-rHuTNF-α). METHODS: The rHuTNF-α was modified with N-succinimidyl succinnate monomethoxy polyethylene glycol (SS-PEG) of three different molecular weights. The PEG-rHuTNF-α was separated into fractions of various molecular weights by gel filtration chromatography. In vitro activities of various fractions were determined with L929 cell assay and in vivo anti-tumor potencies of main fractions were studied with respect to necrosis of S-180 solid tumor. RESULTS: The rHuTNF-α could be modified using SS-PEG under mild conditions. The main fraction of PEG5000-rHuTNF-α contained four PEG molecules, and PEG12000-rHuTNF-α and PEG20000-rHuTNF-α contained two PEG molecules, respectively. There was a higher activity when rHuTNF-α was coupled to less numbers of the same molecular weight PEG molecules. When PEG-rHuTNF-α was of the same molecular weight, rHuTNF-α modified with bigger molecular weight PEG molecules had a higher activity. PEG-rHuTNF-a was resistant to proteolysis, and over 70 % activity remained after 8 h, but the activity of rHuTNF-α was time-dependently diminished by incubation with bovine trypsin. PEG5000-rHuTNF-α (1500 IU per mouse) had a similar anti-tumor potency compared with rHuTNF-a (3000 IU per mouse). PEG12000-rHuTNF-α (1500 IU per mouse) had an in-creased anti-tumor potency compared with rHuTNF-α (3000 IU per mouse). In particular, PEG20000-rHuTNF-α at a dose of 1500 IU per mouse had a higher anti-tumor potency than rHuTNF-α at a dose of 6000 IU per mouse. CONCLUSION: PEG-modified rHuTNF-α could be more suitable for therapeutic use." @default.
- W3141472415 created "2021-04-13" @default.
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- W3141472415 date "2001-01-01" @default.
- W3141472415 modified "2023-09-25" @default.
- W3141472415 title "PEGylated recombinant human tumor necrosis factor alpha: preparation and anti-tumor potency" @default.
- W3141472415 hasPublicationYear "2001" @default.
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