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    [1]
Heart failure    [1]
Hypertension    [2]
Vascular disease    [2]
Drug(s)BenazeprilApprovedHypertension[3][4]
CaptoprilApprovedHypertension[5]
CilazaprilApprovedCongestive heart failure[6]
DeserpidineApprovedHypertension[7][8]
EnalaprilApprovedHypertension[9]
EnalaprilatApprovedHypertension[10]
FosinoprilApprovedHypertension[11]
LisinoprilApprovedHypertension[12]
MoexiprilApprovedHypertension[13]
PerindoprilApprovedHypertension[14]
QuinaprilApprovedHypertension[15]
RamiprilApprovedCongestive heart failure and hypertension[4]
RescinnamineApprovedHypertension[16]
SpiraprilApprovedHypertension[17]
TrandolaprilApprovedHypertension[18]
GSK 796406Suspended in Phase I in GSK 2004 ReportHypertension[19]
IlepatrilDiscontinued in Phase II/IIIHypertension, general; Renal failure; Heart failure; Nephropathy, diabetic[20]
M-100240DiscontinuedHypertension[21]
M100,240DiscontinuedHypertension[21]
OmapatrilatNot approved by FDA due to angioedema safety concernsHypertension[22][23]
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.    
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[24]
ASTRAGALIN[25]
Acetate Ion[24]
BUTEIN[26]
Benazepril[3][4]
CONTIGOSIDE B[25]
Captopril[5]
Cilazapril[6]
Deserpidine[7][8]
Enalapril[9]
Enalaprilat[10]
Fosinopril[11]
GSK 796406[19]
Ilepatril[20]
LY-292223[27]
Lisinopril[12]
M100,240[21]
Moexipril[13]
N-Carboxymethyl-N-cyclopentyl-phthalamic acid[28]
Omapatrilat[22][23]
Perindopril[14]
Perindopril erbumine[14]
Quinapril[15]
RIP[29]
Ramipril[4]
Rescinnamine[16]
SCH-54470[30]
SQ-26332,   SQ-28603[31]
Spirapril[17]
Trandolapril[18]
[Cyclopentyl- (2-nitro-benzoyl)-amino]-acetic acid[28]
kaempferol-3-O- (2''-O-galloyl)-glucoside[25]
MultitargetGSK 796406[19]
Ilepatril[20]
M-100240[21]
Omapatrilat[22][23]
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
Ref 3Efficacy 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 4Nat 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 5Using ACE inhibitors appropriately. Am Fam Physician. 2002 Aug 1;66(3):461-8. To Reference
Ref 6Triple 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 7Angiotensin 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 8Drug interaction exposures in an ambulatory Medicaid population. Am J Hosp Pharm. 1979 Jul;36(7):923-7. To Reference
Ref 9Determination 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 10Analysis of Vancomycin in the Hindlimb Vascular Bed of the Rat. Am J Ther. 1996 Oct;3(10):681-687. To Reference
Ref 11Angiotensin-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 12Involvement 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 13Moexipril 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 14Fixed 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 15An experimental model of encapsulating peritoneal sclerosis. Perit Dial Int. 2009 Feb;29 Suppl 2:S49-50. To Reference
Ref 16Colorimetric determination of indolic drugs. Pak J Pharm Sci. 2005 Apr;18(2):48-51. To Reference
Ref 17Central angiotensin II controls alcohol consumption via its AT1 receptor. FASEB J. 2005 Sep;19(11):1474-81. To Reference
Ref 18Selective 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 19Pipeline of GlaxoSmithKline. GlaxoSmithKline. 2009 To Reference
Ref 20Ilepatril (AVE-7688), a vasopeptidase inhibitor for the treatment of hypertension. Curr Opin Investig Drugs. 2008 Mar;9(3):301-9. To Reference
Ref 21P-74: M100240, a dual ACE/NEP inhibitor, reduces blood pressure in spontaneously hypertensive rats. Am J Hypertens (2002) 15, 59AC59A To Reference
Ref 22Portal 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 23Comparison 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 24Overington 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 25J. Nat. Prod. 50(4):680-683 (1987) To Reference
Ref 26Bioorg 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 27J Med Chem. 2005 Jan 27;48(2):483-98.Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells. To Reference
Ref 28J Med Chem. 1985 Mar;28(3):328-32.Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids. To Reference
Ref 29J Med Chem. 1985 Nov;28(11):1553-5.Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors. To Reference
Ref 30J 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 31J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference



 

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