Therapeutic Targets Database
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TTD Target ID: TTDS00181

Target Information
NameAngiotensin-converting enzyme    
Type of targetSuccessful target    
SynonymsACE    
CD143 antigen    
Dipeptidyl carboxypeptidase I    
Kininase II    
DiseaseChronic obstructive pulmonary disease, unspecified
[ICD9: 460-519, 490-492, 494-496   ICD10: J00-J99, J40-J44, J47]
[1]
Heart failure
[ICD9: 428   ICD10: I50]
[1]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[2]
Vascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[2]
Drug(s)AlaceprilApprovedCardiovascular disease (used to treat hypertension)[3][4][5][6]
BenazeprilApprovedHypertension[7][8]
CaptoprilApprovedHypertension[9]
CilazaprilApprovedCongestive heart failure[10]
DelaprilApprovedCardiovascular disease (essential hypertension)[11][12][5][6][13][14]
DeserpidineApprovedHypertension[15][16]
EnalaprilApprovedHypertension[17]
Enalapril maleateApprovedCardiovascular disease (for the treatment of hypertension and heart failure)[18][19][5][6][13][20][21][22]
EnalaprilatApprovedHypertension[23]
FosinoprilApprovedHypertension[24]
Imidapril hciApprovedCardiovascular disease (used to treat hypertension)[25][26][5][6]
LisinoprilApprovedHypertension[27]
MoexiprilApprovedHypertension[28]
PerindoprilApprovedHypertension[29]
QuinaprilApprovedHypertension[30]
RamiprilApprovedCongestive heart failure and hypertension[8]
RescinnamineApprovedHypertension[31]
SpiraprilApprovedHypertension[32]
Temocapril hydrochlorideApprovedCardiovascular disease (used to treat hypertension)[33][12][5][6]
TrandolaprilApprovedHypertension[34]
GSK 796406Suspended in Phase I in GSK 2004 ReportHypertension[35]
IlepatrilDiscontinued in Phase II/IIIHypertension, general; Renal failure; Heart failure; Nephropathy, diabetic[36]
M-100240DiscontinuedHypertension[37]
M100,240DiscontinuedHypertension[37]
OmapatrilatNot approved by FDA due to angioedema safety concernsHypertension[38][39]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.15.1
PathwayRenin-angiotensin system
UniProt IDP12821
P22966
PDB Structure1O86; 1O8A; 1UZE; 1UZF; 2C6F; 2C6N; 2IUL; 2IUX; 2OC2; 2XY9; 2XYD; 2YDM; 3BKK; 3BKL; 3L3N; 3NXQ; 4APH; 4APJ.    
FunctionConverts angiotensin i to angiotensin ii by release of the terminal his-leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilatator.    
SequenceMGAASGRRGPGLLLPLPLLLLLPPQPALALDPGLQPGNFSADEAGAQLFAQSYNSSAEQV LFQSVAASWAHDTNITAENARRQEEAALLSQEFAEAWGQKAKELYEPIWQNFTDPQLRRI IGAVRTLGSANLPLAKRQQYNALLSNMSRIYSTAKVCLPNKTATCWSLDPDLTNILASSR SYAMLLFAWEGWHNAAGIPLKPLYEDFTALSNEAYKQDGFTDTGAYWRSWYNSPTFEDDL EHLYQQLEPLYLNLHAFVRRALHRRYGDRYINLRGPIPAHLLGDMWAQSWENIYDMVVPF PDKPNLDVTSTMLQQGWNATHMFRVAEEFFTSLELSPMPPEFWEGSMLEKPADGREVVCH ASAWDFYNRKDFRIKQCTRVTMDQLSTVHHEMGHIQYYLQYKDLPVSLRRGANPGFHEAI GDVLALSVSTPEHLHKIGLLDRVTNDTESDINYLLKMALEKIAFLPFGYLVDQWRWGVFS GRTPPSRYNFDWWYLRTKYQGICPPVTRNETHFDAGAKFHVPNVTPYIRYFVSFVLQFQF HEALCKEAGYEGPLHQCDIYRSTKAGAKLRKVLQAGSSRPWQEVLKDMVGLDALDAQPLL KYFQPVTQWLQEQNQQNGEVLGWPEYQWHPPLPDNYPEGIDLVTDEAEASKFVEEYDRTS QVVWNEYAEANWNYNTNITTETSKILLQKNMQIANHTLKYGTQARKFDVNQLQNTTIKRI IKKVQDLERAALPAQELEEYNKILLDMETTYSVATVCHPNGSCLQLEPDLTNVMATSRKY EDLLWAWEGWRDKAGRAILQFYPKYVELINQAARLNGYVDAGDSWRSMYETPSLEQDLER LFQELQPLYLNLHAYVRRALHRHYGAQHINLEGPIPAHLLGNMWAQTWSNIYDLVVPFPS APSMDTTEAMLKQGWTPRRMFKEADDFFTSLGLLPVPPEFWNKSMLEKPTDGREVVCHAS AWDFYNGKDFRIKQCTTVNLEDLVVAHHEMGHIQYFMQYKDLPVALREGANPGFHEAIGD VLALSVSTPKHLHSLNLLSSEGGSDEHDINFLMKMALDKIAFIPFSYLVDQWRWRVFDGS ITKENYNQEWWSLRLKYQGLCPPVPRTQGDFDPGAKFHIPSSVPYIRYFVSFIIQFQFHE ALCQAAGHTGPLHKCDIYQSKEAGQRLATAMKLGFSRPWPEAMQLITGQPNMSASAMLSY FKPLLDWLRTENELHGEKLGWPQYNWTPNSARSEGPLPDSGRVSFLGLDLDAQQARVGQW LLLFLGIALLVATLGLSQRLFSIRHRSLHRHSHGPQFGSEVELRHS
Related US Patent6,133,304
6,337,327
6,482,797
6,509,330
6,521,659
6,555,551
6,586,198
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (Acetylamino)-2-Deoxy-a-D-Glucopyranose[40]
ASTRAGALIN[41]
Acetate Ion[40]
BUTEIN[42]
Benazepril[7][8]
CONTIGOSIDE B[41]
Captopril[9]
Cilazapril[10]
Deserpidine[15][16]
Enalapril[17]
Enalaprilat[23]
Fosinopril[24]
GSK 796406[35]
Ilepatril[36]
LY-292223[43]
Lisinopril[27]
M100,240[37]
Moexipril[28]
N-Carboxymethyl-N-cyclopentyl-phthalamic acid[44]
Omapatrilat[38][39]
Perindopril[29]
Perindopril erbumine[29]
Quinapril[30]
RIP[45]
Ramipril[8]
Rescinnamine[31]
SCH-54470[46]
SQ-26332,   SQ-28603[47]
Spirapril[32]
Trandolapril[34]
[Cyclopentyl- (2-nitro-benzoyl)-amino]-acetic acid[44]
kaempferol-3-O- (2''-O-galloyl)-glucoside[41]
MultitargetGSK 796406[35]
Ilepatril[36]
M-100240[37]
Omapatrilat[38][39]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1ACE in COPD: a therapeutic target? Thorax. 2003 Jul;58(7):556-8. To Reference
Ref 2Aldosterone: a risk factor for vascular disease. Curr Hypertens Rep. 2003 Feb;5(1):59-65. To Reference
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Ref 5Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. To Reference
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Ref 7Efficacy of Benazepril Hydrochloride to Delay the Progression of Occult Dilated Cardiomyopathy in Doberman Pinschers. J Vet Intern Med. 2009 Jul 1. [Epub ahead of print] To Reference
Ref 8Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 9Using ACE inhibitors appropriately. Am Fam Physician. 2002 Aug 1;66(3):461-8. To Reference
Ref 10Triple pharmacological blockade of the renin-angiotensin-aldosterone system in nondiabetic CKD: an open-label crossover randomized controlled trial. Am J Kidney Dis. 2008 Sep;52(3):486-93. Epub 2008 Apr 18. To Reference
Ref 11ARMC 25 To Reference
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Ref 15Angiotensin II-induced modulation of endothelium-dependent relaxation in rabbit mesenteric resistance arteries. J Physiol. 2003 May 1;548(Pt 3):893-906. Epub 2003 Mar 21. To Reference
Ref 16Drug interaction exposures in an ambulatory Medicaid population. Am J Hosp Pharm. 1979 Jul;36(7):923-7. To Reference
Ref 17Determination of bezafibrate, methotrexate, cyclophosphamide, orlistat and enalapril in waste and surface waters using on-line solid-phase extraction liquid chromatography coupled to polarity-switching electrospray tandem mass spectrometry. J Environ Monit. 2009 Apr;11(4):830-8. Epub 2009 Jan 21. To Reference
Ref 18ARMC 20 To Reference
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Ref 20Biodiversity: A continuing source of novel drug leads. Pure Appl. Chem., Vol. 77, No. 1, pp. 724, 2005. by Gordon M. Cragg and David J. Newman To Reference
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Ref 23Analysis of Vancomycin in the Hindlimb Vascular Bed of the Rat. Am J Ther. 1996 Oct;3(10):681-687. To Reference
Ref 24Angiotensin-converting enzyme inhibition and novel cardiovascular risk biomarkers: results from the Trial of Angiotensin Converting Enzyme Inhibition and Novel Cardiovascular Risk Factors (TRAIN) study. Am Heart J. 2009 Feb;157(2):334.e1-8. To Reference
Ref 25ARMC 29 To Reference
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Ref 27Involvement of vascular angiotensin II-forming enzymes in the progression of aortic abdominal aneurysms in angiotensin II- infused ApoE-deficient mice. J Atheroscler Thromb. 2009 Jun;16(3):164-71. Epub 2009 Jun 25. To Reference
Ref 28Moexipril for Treatment of Primary Biliary Cirrhosis in Patients with an Incomplete Response to Ursodeoxycholic Acid. Dig Dis Sci. 2009 Mar 3. [Epub ahead of print] To Reference
Ref 29Fixed combination perindopril-amlodipine (Coveram) in the treatment of hypertension and coronary heart disease. Rev Med Liege. 2009 Apr;64(4):223-7. To Reference
Ref 30An experimental model of encapsulating peritoneal sclerosis. Perit Dial Int. 2009 Feb;29 Suppl 2:S49-50. To Reference
Ref 31Colorimetric determination of indolic drugs. Pak J Pharm Sci. 2005 Apr;18(2):48-51. To Reference
Ref 32Central angiotensin II controls alcohol consumption via its AT1 receptor. FASEB J. 2005 Sep;19(11):1474-81. To Reference
Ref 33ARMC 30 To Reference
Ref 34Selective reduction of central pulse pressure under angiotensin blockage in SHR: role of the fibronectin-alpha5beta1 integrin complex. Am J Hypertens. 2009 Jul;22(7):711-7. Epub 2009 May 7. To Reference
Ref 35Pipeline of GlaxoSmithKline. GlaxoSmithKline. 2009 To Reference
Ref 36Ilepatril (AVE-7688), a vasopeptidase inhibitor for the treatment of hypertension. Curr Opin Investig Drugs. 2008 Mar;9(3):301-9. To Reference
Ref 37P-74: M100240, a dual ACE/NEP inhibitor, reduces blood pressure in spontaneously hypertensive rats. Am J Hypertens (2002) 15, 59AC59A To Reference
Ref 38Portal pressure responses and angiotensin peptide production in rat liver are determined by relative activity of ACE and ACE2. Am J Physiol Gastrointest Liver Physiol. 2009 Jul;297(1):G98-G106. Epub 2009 Apr 23. To Reference
Ref 39Comparison of vasopeptidase inhibitor omapatrilat and angiotensin receptor blocker candesartan on extracellular matrix, myeloperoxidase, cytokines, and ventricular remodeling during healing after reperfused myocardial infarction. Mol Cell Biochem. 2009 Jan;321(1-2):9-22. Epub 2008 Sep 6. To Reference
Ref 40Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 41J. Nat. Prod. 50(4):680-683 (1987) To Reference
Ref 42Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. Epub 2010 Jan 25.The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives. To Reference
Ref 43J Med Chem. 2005 Jan 27;48(2):483-98.Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells. To Reference
Ref 44J Med Chem. 1985 Mar;28(3):328-32.Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids. To Reference
Ref 45J Med Chem. 1985 Nov;28(11):1553-5.Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors. To Reference
Ref 46J Med Chem. 2010 Jan 14;53(1):208-20.Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. To Reference
Ref 47J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference



 

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