Key result
Pepstatylaspartic acid and pepstatylglutamic acid were the most potent competitive inhibitors of porcine renin, with inhibitory constants 2- and 10-fold smaller than pepstatin.
Population
Highly purified pig and human renins acting on the N-acetyltetradecapeptide substrate
Comparison
Four homologues of pepstatin vs Pepstatin
Design
Preclinical
Authors
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These analogs merit preclinical testing in hypertension models; leaves open therapeutic translation for renin inhibition.
Pepstatylglutamic acid and pepstatylaspartic acid are more potent and water-soluble competitive inhibitors of renin compared to pepstatin in vitro.
Eid et al. (1981) studied this question. Pepstatin homologues vs. Pepstatin was evaluated on 50% inhibitory concentrations (IC50) against porcine and human renin. Pepstatylaspartic acid and pepstatylglutamic acid were the most potent competitive inhibitors of porcine renin, with inhibitory constants 2- and 10-fold smaller than pepstatin.
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