Peptide inhibitors of HIV-1 integrase dissociate the enzyme oligomers.

@article{Maroun2001PeptideIO,
  title={Peptide inhibitors of HIV-1 integrase dissociate the enzyme oligomers.},
  author={Richard G. Maroun and St{\'e}phane Gayet and M S Benleulmi and Horea Porumb and Loussin{\'e}e Zargarian and Hayate Merad and Herv{\'e} Leh and Jean François Mouscadet and Fr{\'e}d{\'e}ric Troalen and Serge Fermandjian},
  journal={Biochemistry},
  year={2001},
  volume={40 46},
  pages={13840-8}
}
Integration of HIV-1 genome into host cell chromosome is mediated by viral integrase (IN). The IN catalytic core (CC, IN(50-212)) dimerizes through mutual interactions of its alpha1 and alpha5 helices. Peptides INH1 and INH5 reproducing these helix sequences strongly inhibited IN. For instance, an IC(50) of 80 nM was determined for INH5 in integration assays using wild-type IN (wtIN). In size exclusion chromatography, INH1 and INH5 perturbed the association-dissociation equilibrium of both dmIN… CONTINUE READING
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