Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket

@article{Bai2012CovalentFI,
  title={Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket},
  author={Yu Bai and Huifang Xue and Kun Wang and Lifeng Cai and Jia-yin Qiu and Shuangyu Bi and Luhua Lai and Maosheng Cheng and Shuwen Liu and Keliang Liu},
  journal={Amino Acids},
  year={2012},
  volume={44},
  pages={701-713}
}
Covalent inhibitors form covalent adducts with their target, thus permanently inhibiting a physiological process. Peptide fusion inhibitors, such as T20 (Fuzeon, enfuvirtide) and C34, interact with the N-terminal heptad repeat of human immunodeficiency virus type 1 (HIV-1) gp41 glycoprotein to form an inactive hetero six-helix bundle (6-HB) to prevent HIV-1 infection of host cells. A covalent strategy was applied to peptide fusion inhibitor design by introducing a thioester group into C34-like… 
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