2. Academic Validation
  3. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140

A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140

  • Biochem Biophys Res Commun. 1998 Dec 30;253(3):877-82. doi: 10.1006/bbrc.1998.9871.
H Tamamura 1,  Y Xu,  T Hattori,  X Zhang,  R Arakaki,  K Kanbara,  A Omagari,  A Otaka,  T Ibuka,  N Yamamoto,  H Nakashima,  N Fujii
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, Kyoto University, Japan. tamamura@pharm.kyoto-u.ac.jp
PMID: 9918823 DOI: 10.1006/bbrc.1998.9871
Abstract

T22 ([Tyr5,12, Lys7]-polyphemusin II) is an 18-residue peptide amide, which has strong anti-HIV activity. T22 inhibits the T cell line-tropic (T-tropic) HIV-1 Infection through its specific binding to a Chemokine Receptor CXCR4, which serves as a coreceptor for the entry of T-tropic HIV-1 strains. Herein, we report our finding of novel 14-residue CXCR4 inhibitors, T134 and T140, on the basis of the T22 structure. In the assays we examined, T140 showed the highest inhibitory activity against HIV-1 entry and the strongest inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 among all the CXCR4 inhibitors that have been reported up to now.

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