Design of antiviral stapled peptides containing a biphenyl cross-linker.

Design of antiviral stapled peptides containing a biphenyl cross-linker.
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DOI:
10.1016/j.bmcl.2014.02.038
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发表时间:
2014-04-01
影响因子:
2.7
通讯作者:
Lin, Qing
Lin, Qing
中科院分区:
医学4区
文献类型:
--
作者:
Muppidi, Avinash;Zhang, Hongtao;Curreli, Francesca;Li, Nan;Debnath, Asim K.;Lin, Qing

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Here we report the design and synthesis of a panel of stapled peptides containing a distance-matching biphenyl cross-linker based upon a peptide capsid assembly inhibitor reported previously. Compared with the linear peptide, the biphenyl-stapled peptides exhibited significantly enhanced cell penetration and potent antiviral activity in the cell-based infection assays. Isothermal titration calorimetry and surface plasmon resonance experiments revealed that the most active stapled CAI peptide binds to the C-terminal domain of HIV capsid protein as well as envelop glycoprotein gp120 with low micromolar binding affinities, and as a result, inhibits both the HIV-1 virus entry and the virus assembly.
DOI: 10.1039/c1cc13320a
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期刊: Chemical communications (Cambridge, England)
影响因子: --
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