Experimental Study of Antitumor Activity of Pefagtal Addressed to αvβ3 Integrins

Bull Exp Biol Med. 2022 May;173(1):105-109. doi: 10.1007/s10517-022-05502-6. Epub 2022 May 27.

Abstract

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 αvβ3 and αvβ5 integrins that are predominantly overexpressed in the endothelial cells of tumor blood vessels and in tumor and metastatic cells.

Keywords: drug Pefagtal; metastases; mice tumors; targeted therapy; αvβ3 integrins.

MeSH terms

  • Adenocarcinoma of Lung*
  • Animals
  • Carcinoma, Hepatocellular*
  • Endothelial Cells / metabolism
  • Integrin alphaVbeta3 / metabolism
  • Liver Neoplasms*
  • Mice
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology

Substances

  • Integrin alphaVbeta3
  • Oligopeptides