Angiotensin-converting enzyme
Also known as: ACE, DCP, DCP1
Function
Dipeptidyl carboxypeptidase that removes dipeptides from the C-terminus of a variety of circulating hormones, such as angiotensin I, bradykinin or enkephalins, thereby playing a key role in the regulation of blood pressure, electrolyte homeostasis or synaptic plasticity. Composed of two similar catalytic domains, each possessing a functional active site, with different selectivity for substrates. Plays a major role in the angiotensin-renin system that regulates blood pressure and sodium retention by the kidney by converting angiotensin I to angiotensin II, resulting in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilator, and therefore enhance the blood pressure response. Acts as a regulator of synaptic transmission by mediating cleavage of neuropeptide hormones, such as substance P, neurotensin or enkephalins. Catalyzes degradation of different enkephalin neuropeptides (Met-enkephalin, Leu-enkephalin, Met-enkephalin-Arg-Phe and possibly Met-enkephalin-Arg-Gly-Leu). Acts as a regulator of synaptic plasticity in the nucleus accumbens of the brain by mediating cleavage of Met-enkephalin-Arg-Phe, a strong ligand of Mu-type opioid receptor OPRM1, into Met-enkephalin (By similarity). Met-enkephalin-Arg-Phe cleavage by ACE decreases activation of OPRM1, leading to long-term synaptic potentiation of glutamate release (By similarity). Also acts as a regulator of hematopoietic stem cell differentiation by mediating degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP). Acts as a regulator of cannabinoid signaling pathway by mediating degradation of hemopressin, an antagonist peptide of the cannabinoid receptor CNR1. Involved in amyloid-beta metabolism by catalyzing degradation of Amyloid-beta protein 40 and Amyloid-beta protein 42 peptides, thereby preventing plaque formation. Catalyzes cleavage of cholecystokinin (maturation of Cholecystokinin-8 and Cholecystokinin-5) and Gonadoliberin-1 (both maturation and degradation) hormones. Degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP) and amyloid-beta proteins is mediated by the N-terminal catalytic domain, while angiotensin I and cholecystokinin cleavage is mediated by the C-terminal catalytic region.
Classification
- Family (Pfam)
- PF01401 Peptidase_M2
- InterPro
- Peptidase_M2
- Functional cluster
- Secreted Hydrolases & Toxins
Experimental structures · PDB · 91
- 1O86 X-ray 2.00A
- 1O8A X-ray 2.00A
- 1UZE X-ray 1.82A
- 1UZF X-ray 2.00A
- 2C6F X-ray 3.01A
- 2C6N X-ray 3.00A
- 2IUL X-ray 2.01A
- 2IUX X-ray 2.80A
- 2OC2 X-ray 2.25A
- 2XY9 X-ray 1.97A
- 2XYD X-ray 2.15A
- 2YDM X-ray 2.44A
- … and 79 more
A predicted model is available from AlphaFold.
Gene Ontology · 57
- GO:0005768 endosome
- GO:0009897 external side of plasma membrane
- GO:0070062 extracellular exosome
- GO:0005576 extracellular region
- GO:0005615 extracellular space
- GO:0005764 lysosome
- GO:0005886 plasma membrane
- GO:0003779 actin binding
- GO:0031711 bradykinin receptor binding
- GO:0005516 calmodulin binding
- GO:0031404 chloride ion binding
- GO:0004175 endopeptidase activity
- GO:0008238 exopeptidase activity
- GO:0004181 metallocarboxypeptidase activity
- GO:0070573 metallodipeptidase activity
- GO:0004222 metalloendopeptidase activity
- GO:0008237 metallopeptidase activity
- GO:0051019 mitogen-activated protein kinase binding
- GO:0031434 mitogen-activated protein kinase kinase binding
- GO:0008233 peptidase activity
- GO:0008241 peptidyl-dipeptidase activity
- GO:0008240 tripeptidyl-peptidase activity
- GO:0008270 zinc ion binding
- GO:0050435 amyloid-beta metabolic process
- GO:0002003 angiotensin maturation
- GO:0038166 angiotensin-activated signaling pathway
- GO:0002474 antigen processing and presentation of peptide antigen via MHC class I
- GO:0050482 arachidonate secretion
- GO:0097746 blood vessel diameter maintenance
- GO:0001974 blood vessel remodeling
- GO:0010815 bradykinin catabolic process
- GO:0071838 cell proliferation in bone marrow
- GO:0060047 heart contraction
- GO:0060218 hematopoietic stem cell differentiation
- GO:0042447 hormone catabolic process
- GO:0042445 hormone metabolic process
- GO:0001822 kidney development
- GO:0008584 male gonad development
- GO:0032943 mononuclear cell proliferation
- GO:1903597 negative regulation of gap junction assembly
- GO:0010629 negative regulation of gene expression
- GO:0002446 neutrophil mediated immunity
- GO:0043171 peptide catabolic process
- GO:0003084 positive regulation of systemic arterial blood pressure
- GO:0010608 post-transcriptional regulation of gene expression
- GO:0006508 proteolysis
- GO:0060177 regulation of angiotensin metabolic process
- GO:0008217 regulation of blood pressure
- GO:0086091 regulation of heart rate by cardiac conduction
- GO:1902033 regulation of hematopoietic stem cell proliferation
- GO:0002019 regulation of renal output by angiotensin
- GO:0014910 regulation of smooth muscle cell migration
- GO:0048167 regulation of synaptic plasticity
- GO:0003081 regulation of systemic arterial blood pressure by renin-angiotensin
- GO:0019229 regulation of vasoconstriction
- GO:0007283 spermatogenesis
- GO:0010814 substance P catabolic process
Disease associations
- renal tubular dysgenesis of genetic origin MONDO:0009970
- obsolete susceptibility to ischemic stroke MONDO:0020671
- microvascular complications of diabetes, susceptibility to, 3 MONDO:0012963
- hemorrhage, intracerebral, susceptibility to MONDO:0100533
- OMIM:621420 RAW:OMIM_621420
Drugs targeting this protein · 17
- RAMIPRIL inhibitor
- PERINDOPRIL ERBUMINE inhibitor
- MOEXIPRIL HYDROCHLORIDE inhibitor
- ENALAPRIL MALEATE inhibitor
- SPIRAPRIL HYDROCHLORIDE inhibitor
- QUINAPRIL HYDROCHLORIDE inhibitor
- TRANDOLAPRIL inhibitor
- CAPTOPRIL inhibitor
- BENAZEPRIL HYDROCHLORIDE inhibitor
- FOSINOPRIL SODIUM inhibitor
- IMIDAPRIL inhibitor
- ILEPATRIL inhibitor
- PERINDOPRIL ARGININE inhibitor
- ENALAPRILAT inhibitor
- LISINOPRIL inhibitor
- CILAZAPRIL inhibitor
- DELAPRIL inhibitor
Related proteins · sequence + function similarity
- Angiotensin-converting enzyme 1.00
- Angiotensin-converting enzyme 0.99
- Angiotensin-converting enzyme 0.99
- Angiotensin-converting enzyme 0.99
- Angiotensin-converting enzyme 0.99
- Angiotensin-converting enzyme 0.98
- Angiotensin-converting enzyme 0.98
- Angiotensin-converting enzyme 0.95
- Angiotensin-converting enzyme-like protein Ace3 0.81
- Angiotensin-converting enzyme-related protein 0.78
- Angiotensin-converting enzyme 2 0.74
- Angiotensin-converting enzyme 2 0.73
Co-cited proteins · studied together in the literature
- Progonadoliberin-1 3 shared papers
- Thymosin beta-4 2 shared papers
- Proenkephalin-A 2 shared papers
- Cholecystokinin 2 shared papers
- Angiotensin-converting enzyme 2 5 shared papers
- Kininogen-1 2 shared papers
- Bradykinin-potentiating and C-type natriuretic peptides 1 shared papers
- Angiotensinogen 3 shared papers
- Angiotensin-converting enzyme 2 shared papers
- Amyloid-beta precursor protein 2 shared papers
- Angiotensin-converting enzyme 1 shared papers
- Renin 1 shared papers
Literature · 71 cited papers
- Structural basis of Ac-SDKP hydrolysis by Angiotensin-I converting enzyme. Sci. Rep. · 2015
- Neomorphic effects of recurrent somatic mutations in Yin Yang 1 in insulin-producing adenomas. Proc. Natl. Acad. Sci. U.S.A. · 2015
- Molecular and thermodynamic mechanisms of the chloride-dependent human angiotensin-I-converting enzyme (ACE). J. Biol. Chem. · 2014
- Molecular recognition and regulation of human angiotensin-I converting enzyme (ACE) activity by natural inhibitory peptides. Sci. Rep. · 2012
- ACE as a mechanosensor to shear stress influences the control of its own regulation via phosphorylation of cytoplasmic Ser(1270). PLoS ONE · 2011
- Structural characterization of angiotensin I-converting enzyme in complex with a selenium analogue of captopril. FEBS J. · 2011
- Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
- The N domain of human angiotensin-I-converting enzyme: the role of N-glycosylation and the crystal structure in complex with an N domain-specific phosphinic inhibitor, RXP407. J. Biol. Chem. · 2010
- Abeta42-to-Abeta40- and angiotensin-converting activities in different domains of angiotensin-converting enzyme. J. Biol. Chem. · 2009
- Glycoproteomics analysis of human liver tissue by combination of multiple enzyme digestion and hydrazide chemistry. J. Proteome Res. · 2009
- Hemopressin is an inverse agonist of CB1 cannabinoid receptors. Proc. Natl. Acad. Sci. U.S.A. · 2007
- DNA sequence of human chromosome 17 and analysis of rearrangement in the human lineage. Nature · 2006
- … and 59 more in the literature graph