SYNTHESIS OF Nα-FORMYL-MET-LEU-PHE-OH: AN INDUCER OF CHEMOTAXIS IN PERITONEAL POLYMORPHONUCLEAR NEUTROPHILS

Abstract
A chemotactic peptide CHO.cntdot.Met.cntdot.Leu.cntdot.Phe.cntdot.OH was synthesized classically using the mixed anhydride procedure. The formyl group was introduced by coupling formic acid in the presence of dicyclohexylcarbodiimide to the partially protected tripeptide. The final product was obtained by treatment of the intermediate CHO.cntdot.Met.cntdot.Leu.cntdot.Phe.cntdot.OBzl with HF. The ED50 of the peptide in the Boyden chamber assay was 7 .times. 10-11 M, 2.4 .times. 10-10 M in the lysozyme release assay and 2.6 .times. 10-10 M in the .beta.-glucuronidase release assay. In a radioreceptor assay, the ID50 [median inhibitory dose] of the peptide was 3.3 .times. 10-10 M.