用聚乙二醇对天然人肿瘤坏死因子-α进行化学修饰可增强其抗肿瘤效力。
Chemical modification of natural human tumor necrosis factor-alpha with polyethylene glycol increases its anti-tumor potency.
作者信息
Tsutsumi Y, Kihira T, Yamamoto S, Kubo K, Nakagawa S, Miyake M, Horisawa Y, Kanamori T, Ikegami H, Mayumi T
机构信息
Faculty of Pharmaceutical Sciences, Osaka University.
出版信息
Jpn J Cancer Res. 1994 Jan;85(1):9-12. doi: 10.1111/j.1349-7006.1994.tb02879.x.
Abstract
Natural human tumor necrosis factor-alpha (TNF-alpha) was chemically modified with an active ester of monomethoxy polyethylene glycol (PEG). The molecular weight of PEG-modified TNF-alpha depended on the reaction time as well as the initial molar ratio of PEG to TNF-alpha. The specific activity of modified TNF-alpha was gradually reduced with increase in the degree of PEG-modification, but the plasma half-life of TNF-alpha was increased by up to 40-fold. Modified TNF-alpha showed approximately 100 times greater anti-tumor potency than unmodified TNF-alpha. Covalent attachment of PEG to TNF-alpha thus increased the bioavailability of TNF-alpha, and may facilitate its potential therapeutic use.
摘要
天然人肿瘤坏死因子-α（TNF-α）用单甲氧基聚乙二醇（PEG）的活性酯进行化学修饰。PEG修饰的TNF-α的分子量取决于反应时间以及PEG与TNF-α的初始摩尔比。修饰的TNF-α的比活性随着PEG修饰程度的增加而逐渐降低，但TNF-α的血浆半衰期增加了多达40倍。修饰的TNF-α显示出比未修饰的TNF-α高约100倍的抗肿瘤效力。因此，PEG与TNF-α的共价连接增加了TNF-α的生物利用度，并可能促进其潜在的治疗用途。
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