Enfuvirtide−PEG conjugate: A potent HIV fusion inhibitor with improved pharmacokinetic properties
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- 作者：Shuihong Chenga ; b ; 1 ; Yan Wangc ; 1 ; Zhenxing Zhanga ; d ; Xun Lva ; George F. Gaoa ; e ; Yiming Shaoc ; Liying Mac ; mal@chinaaids.cn" class="auth_mail" title="E-mail the corresponding author ; Xuebing Lia ; b ; e ; lixb@im.ac.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Conjugation ; Enfuvirtide ; Fusion inhibitor ; Human immunodeficiency virus ; Pharmacokinetics ; Poly(ethylene glycol)
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 October 2016
- 年：2016
- 卷：121
- 期：Complete
- 页码：232-237
- 全文大小：828 K
文摘
- 10">
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10">The site-specific conjugation of PEG to a peptide drug enfuvirtide is accomplished.
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15">The conjugate shows similar anti-HIV activity and action mechanism to enfuvirtide.
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The conjugate has better aqueous solubility and longer half-life than enfuvirtide.
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The conjugate inhibits the most common HIV strains circulating in China.