Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.

@article{Christ2010RationalDO,
  title={Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.},
  author={Frauke Christ and Arnout R. D. Voet and Arnaud Marchand and Stefan Nicolet and Belete Ayele Desimmie and Damien Marchand and Doroth{\'e}e Bardiot and Nam Joo Van der Veken and Barbara Van Remoortel and Sergei V. Strelkov and Marc de Maeyer and Patrick Chaltin and Zeger Debyser},
  journal={Nature chemical biology},
  year={2010},
  volume={6 6},
  pages={442-8}
}
Lens epithelium-derived growth factor (LEDGF/p75) is a cellular cofactor of HIV-1 integrase that promotes viral integration by tethering the preintegration complex to the chromatin. By virtue of its crucial role in the early steps of HIV replication, the interaction between LEDGF/p75 and integrase represents an attractive target for antiviral therapy. We have rationally designed a series of 2-(quinolin-3-yl)acetic acid derivatives (LEDGINs) that act as potent inhibitors of the LEDGF/p75… CONTINUE READING
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