PMID: 7034718Aug 1, 1981Paper

New renin inhibitors homologous with pepstatin

The Biochemical Journal
M EidP Corvol

Abstract

Four homologues of pepstatin, the potent but poorly soluble inhibitor of aspartic proteinases, were synthesized by coupling to the C-terminus of the natural pentapeptide the following amino acid residues: L-arginine methyl ester, L-aspartic acid, L-glutamic acid and the dipeptide L-aspartyl-L-arginine. The peptide-coupling reagent we used, benzotriazolyloxytris(dimethylamino)phosphonium hexafluorophosphate, allowed us to obtain readily pure pepstatin homologues with high yields (60-83%). Pepstatylarginine methyl ester and pepstatylglutamic acid were about one order of magnitude more water-soluble than pepstatin. The four homologues and pepstatin were tested in vitro as inhibitors for highly purified pig and human renins acting on the N-acetyltetradecapeptide substrate. The 50% inhibitory concentrations (IC50) of the homologues were ranged from 0.01 to 1 microM against porcine renin at pH 6.0 (pepstatin IC50 approximately 0.32 microM) and from 5.8 to 41 microM against human renin at pH 6.5 (pepstatin IC 50 approximately 17 microM). By three different graphical methods we showed that pepstatin and the four homologues behaved as competitive inhibitors for porcine renin. The most potent inhibitors were pepstatylaspartic acid and pe...Continue Reading

Citations

Jan 1, 1983·Clinical and Experimental Hypertension. Part A, Theory and Practice·E Haber
Apr 1, 1985·American Journal of Kidney Diseases : the Official Journal of the National Kidney Foundation·E Haber
Jun 1, 1982·Bioscience Reports·B M AustenJ Hermon-Taylor
Jun 13, 1986·Biochemical and Biophysical Research Communications·K TakaoriM Donowitz
Nov 1, 1983·Hypertension·E HaberA C Barger
Sep 1, 1991·Hypertension·P Corvol, J Ménard
Apr 1, 1990·Medicinal Research Reviews·W J Greenlee

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