Target intelligence / Profile preview

Angiotensin-converting enzyme 1 (ACE1 (commonly abbreviated as ACE, but ACE1 used to distinguish from ACE2))

Target
ACE1 (commonly abbreviated as ACE, but ACE1 used to distinguish from ACE2)
Molecular classification
Enzyme, Metalloprotease, Zinc- and chloride-dependent peptidase, Membrane-bound enzyme
01

Overview

Angiotensin-converting enzyme 1 is a zinc- and chloride-dependent metalloprotease that plays a central role in the renin–angiotensin–aldosterone system by converting the inactive precursor angiotensin I to the potent vasoconstrictor angiotensin II, thereby regulating blood pressure, electrolyte homeostasis, and vascular tone. ACE1 is a type I membrane-bound glycoprotein mainly expressed in vascular endothelial, renal, and pulmonary tissues, and is targeted therapeutically in cardiovascular and renal diseases by ACE inhibitors, which lower blood pressure and decrease cardiovascular risk. It also degrades bradykinin, a vasodilator, and thus modulates pathways implicated in both blood pressure and inflammatory responses. Excess ACE activity is associated with hypertension, heart failure, and renal pathologies, making ACE1 inhibition a widely used therapeutic intervention in these diseases.

Other names
ACEAngiotensin-converting enzymeKininase IIDipeptidyl carboxypeptidase IPeptidyl-dipeptidase A
02

Mechanism of action

Inhibition of conversion of angiotensin I to angiotensin II; Inhibition of degradation of bradykinin; Decrease in vasoconstriction, leading to vasodilation; Reduction of aldosterone secretion; Lowering of blood pressure and reduced cardiac workload.

03

Biological functions

Blood pressure regulationConversion of angiotensin I to angiotensin IIDegradation of bradykininElectrolyte and fluid homeostasisRegulation of vascular tone
04

Disease associations

Cardiovascular diseaseHypertensionHeart failureChronic kidney diseaseDiabetes (renal complications)Vascular diseaseRenal impairment
05

Safety considerations

Cough (related to bradykinin accumulation)AngioedemaHyperkalemiaHypotensionRenal impairment (especially in patients with bilateral renal artery stenosis)Teratogenicity (contraindicated in pregnancy)
06

Interacting drugs

Captopril

9 more in the full profile.

07

Biomarkers

Plasma ACE activity (for sarcoidosis, not typically for efficacy monitoring)Plasma renin activityBlood pressure (clinical biomarker of pharmacodynamic effect)

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