Tuftsin: its chemistry, biology, and clinical potential

Tuftsin is a tetrapeptide, Thr-Lys-Pro-Arg, which resides in the Fc-domain of the heavy chain of immunoglobulin G. The peptide originates from a specific fraction of the parent protein through enzymatic processing. Tuftsin possesses a broad spectrum of activities related primarily to the immune system function and exerts on phagocytic cells, notably on macrophages. These include potentiation of various cell functions such as phagocytosis, motility, immunogenic response, and bactericidal and tumoricidal activities. The features of tuftsin, coupled with its low toxicity, make the peptide an attractive candidate for immunotherapy. Tuftsin's capacity to augment cellular activation is mediated by specific receptors that were identified, characterized, and recently isolated from rabbit peritoneal granulocytes. Tuftsin has been chemically synthesized by a variety of techniques, some of which are adequate for large-scale preparations. A multitude of analogs have also been synthesized and extensively studied for structure-function relationships.