Abstract |
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.
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Authors | Mati Fridkin, Haim Tsubery, Esther Tzehoval, Ami Vonsover, Laura Biondi, Fernando Filira, Raniero Rocchi |
Journal | Journal of peptide science : an official publication of the European Peptide Society
(J Pept Sci)
Vol. 11
Issue 1
Pg. 37-44
(Jan 2005)
ISSN: 1075-2617 [Print] England |
PMID | 15635725
(Publication Type: Journal Article)
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Copyright | Copyright (c) 2004 European Peptide Society and John Wiley & Sons, Ltd. |
Chemical References |
- Anti-HIV Agents
- Drug Carriers
- Interleukin-1
- Reverse Transcriptase Inhibitors
- tuftsin-AZT conjugate
- Zidovudine
- HIV Reverse Transcriptase
- Tuftsin
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Topics |
- Animals
- Anti-HIV Agents
(pharmacology, toxicity)
- Antigen Presentation
- Cell Line
- Cell Survival
(drug effects)
- Cells, Cultured
- Drug Carriers
- Drug Design
- Female
- HIV Reverse Transcriptase
(antagonists & inhibitors, metabolism)
- HIV-1
(drug effects, physiology)
- Humans
- Interleukin-1
(metabolism)
- Macrophages
(drug effects, immunology, virology)
- Mice
- Reverse Transcriptase Inhibitors
(pharmacology, toxicity)
- Tuftsin
(analogs & derivatives, chemical synthesis, pharmacology, toxicity)
- Virus Replication
(drug effects)
- Zidovudine
(analogs & derivatives, chemical synthesis, pharmacology, toxicity)
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