Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes.

@article{Tamamura2000PharmacophoreIO,
  title={Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes.},
  author={Hirokazu Tamamura and Akane Omagari and Shinya Oishi and Taisei Kanamoto and Naoki Yamamoto and Stephen C. Peiper and Hideki Nakashima and Akira Otaka and Nobutaka Fujii},
  journal={Bioorganic & medicinal chemistry letters},
  year={2000},
  volume={10 23},
  pages={2633-7}
}
A polyphemusin peptide analogue, T22 ([Tyr(5,12), Lys7]-polyphemusin II), and its shortened potent analogues, T134 (des-[Cys(8,13), Tyr(9,12)]-[D-Lys10, Pro11, L-citrulline16]-T22 without C-terminal amide) and T140 [[L-3-(2-naphthyl)alanine3]-T134], strongly inhibit the T-cell line-tropic (T-tropic) HIV-1 infection through their specific binding to a chemokine receptor, CXCR4. T22 is an extremely basic peptide possessing five Arg and three Lys residues in the molecule. In our previous study, we… CONTINUE READING

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