کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1357694 | 981273 | 2016 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design, synthesis and activity evaluation of novel peptide fusion inhibitors targeting HIV-1 gp41 Design, synthesis and activity evaluation of novel peptide fusion inhibitors targeting HIV-1 gp41](/preview/png/1357694.png)
Human immunodeficiency virus type 1 (HIV-1), the pathogen of acquired immunodeficiency syndrome (AIDS), causes about 2 million people to death every year. Fusion inhibitors targeted the envelope protein (gp41) represent a novel and alternative approach for anti-AIDS therapy, which terminates the HIV-1 life cycle at an early stage. Using CP621-652 as a template, a series of peptides were designed, synthesized and evaluated in vitro assays. An interesting phenomenon was found that the substitution of hydrophobic residues at solvent accessible sites could increase the anti-HIV activity when the C-terminal sequence was extended with an enough numbers of amino acids. After the active peptides was synthesized and evaluated, peptide 8 showed the best anti-HIV-1 IIIB whole cell activity (MAGI IC50 = 53.02 nM). Further study indicated that peptide 8 bound with the gp41 NHR helix, and then blocked the conformation of 6-helix, thus inhibited virus–cell membrane fusion. The results would be helpful for the design of peptide fusion inhibitors against HIV-1 infection.
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Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 2, 15 January 2016, Pages 201–206