Key result
Modification of a 13-membered-ring glutamine-derived inhibitor at P4 led to a macrocyclic renin inhibitor with an IC50 of 56 nM.
Population
Computer model of the active site of human renin and in vitro assays
Design
Preclinical
Authors
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Should not yet change clinical practice; supports macrocyclic renin inhibitor design efforts.
The study demonstrates the viability of designing macrocyclic renin inhibitors with a scissile-bond replacement, achieving nanomolar inhibitory potency in vitro.
Weber et al. (1991) studied this question. P2-P1'-linked macrocyclic renin inhibitors was evaluated on IC50 for renin inhibition. Modification of a 13-membered-ring glutamine-derived inhibitor at P4 led to a macrocyclic renin inhibitor with an IC50 of 56 nM.
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