Background: Immunomodulation is one of the significant therapeutic strategies. It
includes both stimulation and suppression of the immune system by a variety of substances called
immunomodulators, designed to regulate the immune response of the organism against infections
of varying etiology. An example of such a substance is tuftsin (TKPA) 3 (Fig. (1)). In this paper
were included tuftsin derivatives, which were described over the years, their together with biological
activity and clinical potential.
Methods: We reviewed a bibliographic database to gather all the important information about the
tuftsin peptide. We have delineated the significant information on the activity of the tetrapeptide
itself and its derivatives. Analogs were divided because of their anti-tumor, anti-inflammatory,
antimicrobial and anti-viral activity.
Results: This paper describes eighty-six documents. Thirty-two of them concern on activity of
tuftsin in the human organism. The remaining fifty-four describe peptide analogues and their
properties, including eleven papers about the tuftsin-based peptides contained in the vaccines,
nine papers representing anticancer activity of the tuftsin derivatives, twenty-six about antiinflammatory
compounds, and five papers describing the antitumor activity of the tuftsin analogs.
Conclusion: The findings of this review confirm the importance of the tuftsin and their derivatives.
Most of these substances showed anti-tumor, anti-inflammatory or antibacterial activities.
A large amount of the compounds may find use in vaccines. Tuftsin can also be used to prepare
fusion proteins in the treatment of cancer and as carriers of many biologically active substances.