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Biochemical pharmacology

Mixed-type inhibition of bovine lung angiotensin converting enzyme by lisinopril and its dansyl derivative.


PMID 1324678

Abstract

The steady-state inhibition of bovine lung angiotensin converting enzyme (ACE; EC 3.4.15.1) by the slow-binding inhibitor lisinopril and its dansyl derivative conformed to a linear mixed inhibition model with inhibitor binding to ES as well as to E. Studied at pH8, 35 degrees, and using N-(3-[2-furyl]-acryloyl)phe-gly-gly as substrate, the approach to steady-state activity at different substrate concentrations pointed to slow isomerizations in both EI and EIS. While an inhibitory scheme involving a single I-binding site adequately accounts for the data presented, information relating to the primary structure of ACE brings up a two-site alternative which remains to be tested.

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F7131
N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly
C20H21N3O6