Cyclic peptide inhibitors of HIV-1 integrase derived from the LEDGF/p75 protein.

@article{Hayouka2010CyclicPI,
  title={Cyclic peptide inhibitors of HIV-1 integrase derived from the LEDGF/p75 protein.},
  author={Zvi Hayouka and Mattan Hurevich and Aviad Levin and Hadar Benyamini and Anat Iosub and Michal Maes and Deborah E. Shalev and Abraham Loyter and Chaim Gilon and Assaf Friedler},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 23},
  pages={8388-95}
}
Restricting linear peptides to their bioactive conformation is an attractive way of improving their stability and activity. We used a cyclic peptide library with conformational diversity for selecting an active and stable peptide that mimics the structure and activity of the HIV-1 integrase (IN) binding loop from its cellular cofactor LEDGF/p75 (residues 361-370). All peptides in the library had the same primary sequence, and differed only in their conformation. Library screening revealed that… CONTINUE READING

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Synthesis of Cyclic Peptides, In Houben–Weyl: Methods of Organic Chemistry, Synthesis of Peptides

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