Experimental Study of Antitumor Activity of Pefagtal Addressed to [alpha]v[beta]3 Integrins

We studied the effect of a new targeted drug Pefagtal that represents a conjugate in which the MS2 phage filled with a substance toxic to cells (thallium salts) is covalently linked to peptides containing the RGD motif. The antitumor and pronounced antimetastatic effects of Pefagtal were demonstrated on transplanted mouse tumors differing in histological type and status of metastasis: Krebs-2 ascites adenocarcinoma of the mammary gland, Lewis lung adenocarcinoma, hepatoma-29, and lung adenocarcinoma. It is assumed that the RGD motif mediates primary binding of the construct to [alpha]v[beta]3 and [alpha]v[beta]5 integrins that are predominantly overexpressed in the endothelial cells of tumor blood vessels and in tumor and metastatic cells. Key Words: mice tumors; metastases; [alpha]v[beta]3 integrins; targeted therapy; drug Pefagtal