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Tuftsin‐AZT conjugate: potential macrophage targeting for AIDS therapy
Author(s) -
Fridkin Mati,
Tsubery Haim,
Tzehoval Esther,
Vonsover Ami,
Biondi Laura,
Filira Fernando,
Rocchi Raniero
Publication year - 2005
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.587
Subject(s) - tuftsin , conjugate , peptide , chimera (genetics) , chemistry , receptor , cytotoxic t cell , internalization , virology , pharmacology , microbiology and biotechnology , biology , immunology , in vitro , biochemistry , mathematical analysis , mathematics , gene
The IgG‐derived immunomodulating peptide tuftsin, Thr‐Lys‐Pro‐Arg, is recognized by specific receptors on phagocytic cells, notably macrophages, and is capable of targeting proteins and peptides to these sites. Aiming to target 3′‐azido‐3′‐deoxythymidine (AZT) to HIV‐infected macrophages, a conjugate of AZT with tuftsin was synthesized. The AZT‐tuftsin chimera possesses the characteristic capacities of its two components. Thus, like AZT, it inhibits reverse transcriptase activity and HIV‐antigen expression, and similarly to tuftsin, it stimulates IL‐1 release from mouse macrophages and augments the immunogenic function of the cells. Importantly, the conjugate is not cytotoxic to T‐cells. The results suggest that the AZT‐tuftsin conjugate might have potential use in AIDS therapy. Copyright © 2004 European Peptide Society and John Wiley & Sons, Ltd.