Structure-function analysis of angiotensin I-converting enzyme using monoclonal antibodies. Selective inhibition of the amino-terminal active site.

Angiotensin Converting Enzyme in Sarcoidosis

Selective angiotensin-converting enzyme C-domain inhibition is sufficient to prevent angiotensin I-induced vasoconstriction.

Somatic angiotensin-converting enzyme (ACE) contains 2 domains (C-domain and N-domain) capable of hydrolyzing angiotensin I (Ang I) and bradykinin. Here we investigated the effect of the selective C-domain and N-domain inhibitors RXPA380 and RXP407 on Ang I-induced vasoconstriction of porcine femoral arteries (PFAs) and bradykinin-induced vasodilation of preconstricted porcine coronary microart...

Angiotensin I converting enzyme.

• Interest in particular biologically active substances waxes and wanes. Investigators rush into a newly opened field, solve a few problems, and frequently raise more; then they rush out to follow more promising developments elsewhere. However, interest in angiotensins generally has persisted and increased. Observation of the actions of angiotensins has led to the study of enzymes involved in t...

Development of domain-selective angiotensin I-converting enzyme inhibitors.

Somatic angiotensin-converting enzyme (ACE) is an essential component of the renin-angiotensin system and consequently plays a key role in blood pressure and electrolyte homeostasis. Thus, ACE inhibitors are widely used in the treatment of cardiovascular disease, causing a decrease in the production of angiotensin II and an increase in the circulating vasodilator bradykinin. The ectodomain of A...

Mechanism-Based Studies of the Active Site-Directed Inhibition and Activation of Enzyme Transketolase

Derivatives of phenyl-keto butenoic acids have been reported to be inhibitors of pyruvate decarboxylase, (PDC). The inhibition of transketolase, a thiamine requiring enzyme such as PDF, by meta nitrophenyl derivative of 2-oxo-3-butenoic acid (MNPB) is reported here. These studies indicate that the inhibitor binds to the enzyme at the active site. A two-step inhibition was observed, first th...