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Structural basis for the inhibition of human angiotensin-1 converting enzyme by fosinoprilat.


ABSTRACT: Human angiotensin I-converting enzyme (ACE) has two isoforms, somatic ACE (sACE) and testis ACE (tACE). The functions of sACE are widespread, with its involvement in blood pressure regulation most extensively studied. sACE is composed of an N-domain (nACE) and a C-domain (cACE), both catalytically active but have significant structural differences, resulting in different substrate specificities. Even though ACE inhibitors are used clinically, they need much improvement because of serious side effects seen in patients (~ 25-30%) with long-term treatment due to nonselective inhibition of nACE and cACE. Investigation into the distinguishing structural features of each domain is therefore of vital importance for the development of domain-specific inhibitors with minimal side effects. Here, we

SUBMITTER: Cozier GE 

PROVIDER: S-EPMC9796954 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature