Peptide Fragment 66--77 of Monocyte Chemoattractant Protein 1 and Its retro-enantio Analogue Inhibit the Migration of Cells In Vitro and In Vivo

M. V. Sidorova, ^# A. S. Molokoedov , A. A. Az'muko , T. I. Aref'eva , M. G. Melekhov , N. B. Kukhtina , T. L. Krasnikova , Zh . D. Bespalova , and V. N. Bushuev

^# Phone: +7 (495) 414-6716; e-mail: peptide@cardio.ru

Russian Cardiological Research and Production Association, Federal Agency for Healthcare and Social Development, Tret'ya Cherepkovskaya ul. 15a, Moscow , 121552 Russia

Received July 11, 2005; in final form, October 3, 2005

Abstract: The retro-enantio analogue of peptide 66--77 of the chemokine MCP-1 and two hexapeptide fragments 66--71 and 72--77 of the C-terminal sequence of this protein were synthesized using the Fmoc strategy of solid phase peptide synthesis. The effect of the synthetic peptides upon the MCP-1--stimulated migration of THP-1 mononuclear cells was studied in vitro. The activity of the retro-enantio analogue was found to be comparable with that of the initial peptide 66--77: both peptides inhibit the migration of monocytes and granulocytes into inflammation zones of experimental animals.

Key words: MCP-1--stimulated cell migration, monocyte, monocyte chemoattractant protein 1 (MCP-1), solid phase peptide synthesis, synthetic peptides, transpeptidation

Russian Journal of Bioorganic Chemistry 2006, 32 (2):146-153