Angiotensin-converting enzyme

Nomenclature: Angiotensin-converting enzyme

Abbreviated Name: ACE1

Family: M2: Angiotensin-converting enzyme peptidase unit 1

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Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1306 17q23.3 ACE angiotensin I converting enzyme
Mouse - 1312 11 E1 Ace angiotensin I converting enzyme (peptidyl-dipeptidase A) 1
Rat - 1313 10q32.1 Ace angiotensin I converting enzyme
Previous and Unofficial Names
ACE
Dipeptidyl carboxypeptidase I
Kininase II
CD143
DCP1
ACE1
StsRR92
Dipeptidyl carboxypeptidase 1
Dipeptidyl carboxypeptidase 1 (Angiotensin I-converting enzyme)
angiotensin 1 converting enzyme
angiotensin 1 converting enzyme 1
angiotensin I converting enzyme 1
angiotensin I-converting enzyme (Dipeptidyl carboxypeptidase 1)
angiotensin converting enzyme
angiotensin-converting enzyme
angiotensin I converting enzyme (peptidyl-dipeptidase A) 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
MEROPS
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Enzyme Reaction
EC Number: 3.4.15.1
Endogenous substrates (Human)
angiotensin I (AGT, P01019) > angiotensin II (AGT, P01019)
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
lisinopril Hs Inhibition 9.4 pKi 11
pKi 9.4 (Ki 3.6x10-10 M) [11]
zofenoprilat Oc Inhibition 9.4 pKi 8
pKi 9.4 (Ki 4x10-10 M) [8]
captopril Hs Inhibition 8.4 pKi 11
pKi 8.4 (Ki 3.98x10-9 M) [11]
fasidotrilat Hs Inhibition 8.0 pKi 1
pKi 8.0 (Ki 9.8x10-9 M) [1]
spiraprilat Hs Inhibition 9.1 pIC50 13
pIC50 9.1 (IC50 8x10-10 M) [13]
perindoprilat Hs Inhibition 9.0 pIC50 2
pIC50 9.0 (IC50 1.05x10-9 M) [2]
benazepril Hs Inhibition 8.8 pIC50 14
pIC50 8.8 (IC50 1.7x10-9 M) [14]
cilazaprilat Oc Inhibition 8.7 pIC50 15
pIC50 8.7 (IC50 1.9x10-9 M) [15]
imidaprilat Hs Inhibition 8.7 pIC50 12
pIC50 8.7 (IC50 2x10-9 M) [12]
trandolaprilat Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3.2x10-9 M) [3]
quinoprilat Hs Inhibition 8.5 pIC50 6
pIC50 8.5 (IC50 2.9x10-9 M) [6]
ramiprilat Hs Inhibition 8.4 pIC50 10
pIC50 8.4 (IC50 4.2x10-9 M) [10]
moexiprilat Oc Inhibition 8.2 pIC50 5
pIC50 8.2 (IC50 6.5x10-9 M) [5]
zofenoprilat Rn Inhibition 8.1 pIC50 8
pIC50 8.1 (IC50 8x10-9 M) [8]
quinapril Cp Inhibition 8.1 pIC50 7
pIC50 8.1 (IC50 8.3x10-9 M) [7]
fosinoprilat Oc Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1.1x10-8 M) [4]
trandolapril Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.5x10-8 M) [3]
ramipril Hs Inhibition 7.6 pIC50 10
pIC50 7.6 (IC50 2.6x10-8 M) [10]
enalaprilat Hs Inhibition 7.5 pIC50 3
pIC50 7.5 (IC50 3.4x10-8 M) [3]
benazeprilat Hs Inhibition 6.6 pIC50 9
pIC50 6.6 (IC50 2.8x10-7 M) [9]
enalapril Hs Inhibition 4.3 pIC50 3
pIC50 4.3 (IC50 5x10-5 M) [3]
spirapril Hs Inhibition - -
fosinopril Hs Inhibition - -
moexipril Hs Inhibition - -
imidapril Hs Inhibition - -
perindopril Hs Inhibition - -
fasidotril Hs Inhibition - -
zofenopril Hs Inhibition - -
cilazapril Hs Inhibition - -
View species-specific inhibitor tables
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0000530 abnormal kidney vasculature morphology PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0000208 decreased hematocrit PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0003918 decreased kidney weight PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0006264 decreased systemic arterial systolic blood pressure PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0002988 decreased urine osmolality PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0003675 kidney cysts PMID: 12637363 
Acetm4Keb|Bdkrb2tm1Jfh Acetm4Keb/Acetm4Keb,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S1/Sv * 129S7/SvEvBrd * 129X1/SvJ
MGI:102845  MGI:87874  MP:0001864 vasculitis PMID: 12637363 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Stroke, hemorrhagic
OMIM:  614519
References: 
Mutations not determined
Disease:  Microvascular complications of diabetes, susceptibility to, 3
OMIM:  612624
References: 
Mutations not determined
Disease:  Renal tubular dysgenesis
OMIM:  267430
Orphanet:  97369
References: 
Mutations not determined

The Guide to PHARMACOLOGY curates quantitative bioactivity mappings for all approved, clinical and selected actively pursued research targets. Data for additional protein mappings from medicinal chemistry papers and selected PubChem Bioassays can be found in the ChEMBL links.

References

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1. Abbenante G, Fairlie DP. (2005) Protease inhibitors in the clinic. Med Chem1 (1): 71-104. [PMID:16789888]

2. Ceconi C, Francolini G, Olivares A, Comini L, Bachetti T, Ferrari R. (2007) Angiotensin-converting enzyme (ACE) inhibitors have different selectivity for bradykinin binding sites of human somatic ACE. Eur. J. Pharmacol.577 (1-3): 1-6. [PMID:17716647]

3. Chevillard C, Jouquey S, Bree F, Mathieu MN, Stepniewski JP, Tillement JP, Hamon G, Corvol P. (1994) Compared properties of trandolapril, enalapril, and their diacid metabolites. J. Cardiovasc. Pharmacol.23 Suppl 4: S11-5. [PMID:7527095]

4. DeForrest JM, Waldron TL, Harvey C, Scalese B, Rubin B, Powell JR, Petrillo EW, Cushman DW. (1989) Fosinopril, a phosphinic acid inhibitor of angiotensin I converting enzyme: in vitro and preclinical in vivo pharmacology. J. Cardiovasc. Pharmacol.14 (5): 730-6. [PMID:2481187]

5. Friehe H, Ney P. (1997) Pharmacological and toxicological studies of the new angiotensin converting enzyme inhibitor moexipril hydrochloride. Arzneimittelforschung47 (2): 132-44. [PMID:9079232]

6. Hausin RJ, Codding PW. (1991) Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors. J. Med. Chem.34 (2): 511-7. [PMID:1995872]

7. Kaplan HR, Cohen DM, Essenburg AD, Major TC, Mertz TE, Ryan MJ. (1984) CI-906 and CI-907: new orally active nonsulfhydryl angiotensin-converting enzyme inhibitors. Fed. Proc.43 (5): 1326-9. [PMID:6323223]

8. Krapcho J, Turk C, Cushman DW, Powell JR, DeForrest JM, Spitzmiller ER, Karanewsky DS, Duggan M, Rovnyak G, Schwartz J et al.. (1988) Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines. J. Med. Chem.31 (6): 1148-60. [PMID:2836590]

9. Lefebvre HP, Brown SA, Chetboul V, King JN, Pouchelon JL, Toutain PL. (2007) Angiotensin-converting enzyme inhibitors in veterinary medicine. Curr. Pharm. Des.13 (13): 1347-61. [PMID:17506720]

10. Metzger H, Maier R, Sitter C, Stern HO. (1984) 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S,5S) -2-azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498)--a new and highly effective angiotensin I converting enzyme inhibitor. Arzneimittelforschung34 (10B): 1402-6. [PMID:6097265]

11. Michaud A, Williams TA, Chauvet MT, Corvol P. (1997) Substrate dependence of angiotensin I-converting enzyme inhibition: captopril displays a partial selectivity for inhibition of N-acetyl-seryl-aspartyl-lysyl-proline hydrolysis compared with that of angiotensin I. Mol. Pharmacol.51 (6): 1070-6. [PMID:9187274]

12. Robinson DM, Curran MP, Lyseng-Williamson KA. (2007) Imidapril: a review of its use in essential hypertension, Type 1 diabetic nephropathy and chronic heart failure. Drugs67 (9): 1359-78. [PMID:17547476]

13. Smith EM, Swiss GF, Neustadt BR, McNamara P, Gold EH, Sybertz EJ, Baum T. (1989) Angiotensin converting enzyme inhibitors: spirapril and related compounds. J. Med. Chem.32 (7): 1600-6. [PMID:2544729]

14. Stanton JL, Watthey JW, Desai MN, Finn BM, Babiarz JE, Tomaselli HC. (1985) Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives. J. Med. Chem.28 (11): 1603-6. [PMID:2999394]

15. Waterfall JF. (1989) A review of the preclinical cardiovascular pharmacology of cilazapril, a new angiotensin converting enzyme inhibitor. Br J Clin Pharmacol27 Suppl 2: 139S-150S. [PMID:2527528]

How to cite this page

M2: Angiotensin-converting enzyme peptidase unit 1: Angiotensin-converting enzyme. Last modified on 06/05/2014. Accessed on 31/07/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1613.