Therapeutic Targets Database
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TTD Target ID: TTDS00267

Target Information
NameType-1 angiotensin II receptor    
Type of targetSuccessful target    
SynonymsAT1    
AT1AR    
Angiotensin 1 receptor    
Angiotensin II receptor 1    
DiseaseCardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[1]
Heart failure
[ICD9: 428   ICD10: I50]
[2]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[3]
Ischemic stroke
[ICD9: 434.91   ICD10: I61-I63]
[4]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[5]
Drug(s)CandesartanApprovedHypertension[6][1]
EprosartanApprovedHypertension[7]
Eprosartan mesylateApprovedHigh blood pressure[8]
ForasartanApprovedHypertension[9][10]
IrbesartanApprovedHypertension[11]
LosartanApprovedHypertension[11][12][13]
OlmesartanApprovedHypertension[14]
Olmesartan medoxomilApprovedHigh blood pressure[15]
SaprisartanApprovedHypertension[16]
TasosartanApprovedHypertension[17]
TelmisartanApprovedHypertension[18]
ValsartanApprovedHypertension[11][12]
S-474474Phase IIIMetabolic Syndrome[19]
TAK-591Phase IHypertension[20]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Renin-angiotensin system
Vascular smooth muscle contraction
UniProt IDP30556
PDB Structure1ZV0.    
FunctionReceptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system.    
SequenceMILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLK TVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLT CLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVC AFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFK IIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPL FYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE
Related US Patent6,300,356
6,544,968
6,589,547
6,638,937
6,641,811
6,767,905
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor4- (2-Butyl-benzoimidazol-1-ylmethyl)-phenol[21]
ANGIOTENSIN II[22]
BMS-248360[23]
CV-11194[24]
Carboxylic Acid Metabolite (E-3174)[25]
GNF-PF-2307[26]
GNF-PF-2812[26]
GNF-PF-3832[26]
HELENALIN[26]
L-159093[23]
L-159689[23]
L-162313[27]
L-162782[27]
SARALASIN[28]
TAK-536[24]
[Bpa1]AngII[22]
[Sar1,Bpa2]AngII[22]
[Sar1,Bpa3]AngII[22]
[Sar1,Bpa8]AngII[22]
[Sar1,Tdf2]AngII[22]
[Sar1,Tdf3]AngII[22]
[Sar1,Tdf8]AngII[22]
[Tdf1]AngII[22]
Antagonist (E)-N-[29]
4-[ (diphenylmethyl)amino]-2-phenylquinazoline[30]
4-hydroxy-1-methyl-4- (4-methylphenyl)-3-piperidyl 4-methylphenyl ketone[31]
Candesartan[6][1]
Eprosartan[7]
Eprosartan mesylate[8]
Forasartan[9][10]
GBR-12935[32]
Irbesartan[11]
Losartan[11][12][13]
Olmesartan[14]
Olmesartan medoxomil[15]
RTI-76[33]
Saprisartan[16]
TAK-591[20]
Tasosartan[17]
Telmisartan[18]
Valsartan[11][12]
BlockerS-474474[19]
MultitargetTAK-591[20]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Angiotensin II type 1 receptor blockade: a novel therapeutic concept. Blood Press Suppl. 2000;1:9-13. To Reference
Ref 2Angiotensin I receptor blockers for heart failure. Wien Med Wochenschr. 2001;151(7-8):157-9. To Reference
Ref 3Angiotensin III: a central regulator of vasopressin release and blood pressure. Trends Endocrinol Metab. 2001 May-Jun;12(4):157-62. To Reference
Ref 4Cerebral ischemia enhances vascular angiotensin AT1 receptor-mediated contraction in rats. Stroke. 2004 Apr;35(4):970-4. Epub 2004 Mar 4. To Reference
Ref 5Oxidative stress and antioxidant therapy in Parkinson's disease. Prog Neurobiol. 1996 Jan;48(1):1-19. To Reference
Ref 6Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. To Reference
Ref 7Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7. To Reference
Ref 8The angiotensin receptor blocker eprosartan mesylate reduces pulse pressure in isolated systolic hypertension. Can J Cardiol. 2004 Oct;20 Suppl C:11C-16C. To Reference
Ref 9Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J Med Chem. 2003 Feb 27;46(5):716-26. To Reference
Ref 10Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001 Aug;86(4):381-9. To Reference
Ref 11Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41. To Reference
Ref 12Nat 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 13Effect of episodic hypoxia on sympathetic activity and blood pressure. Respir Physiol. 2000 Feb;119(2-3):189-97. To Reference
Ref 14A case of Henoch-Sch?nlein purpura nephritis successfully treated with tonsillectomy and steroid pulse therapy. Nippon Jinzo Gakkai Shi. 2009;51(4):484-9. To Reference
Ref 15Mechanism of diastolic stiffening of the failing myocardium and its prevention by angiotensin receptor and calcium channel blockers. J Cardiovasc Pharmacol. 2009 Jul;54(1):47-56. To Reference
Ref 16Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F. To Reference
Ref 17Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54. To Reference
Ref 18Deletion of angiotensin II type I receptor reduces hepatic steatosis. J Hepatol. 2009 Jun;50(6):1226-35. Epub 2009 Mar 11. To Reference
Ref 192011 Pipeline of Shionogi. To Reference
Ref 20Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 21Bioorg. Med. Chem. Lett. 4(1):213-218 (1994) To Reference
Ref 22J Med Chem. 2010 Mar 11;53(5):2063-75.The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1. To Reference
Ref 23J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. To Reference
Ref 24J Med Chem. 1996 Dec 20;39(26):5228-35.Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres. To Reference
Ref 25Bioorg. Med. Chem. Lett. 4(1):177-182 (1994) To Reference
Ref 26Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 27Bioorg Med Chem. 2008 Jul 15;16(14):6841-9. Epub 2008 Jul 1.Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships. To Reference
Ref 28J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. To Reference
Ref 29Pharmacological characterization of (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n ortropane as a selective and potent inhibitor of the neuronal dopamine transporter. J Pharmacol Exp Ther. 1999 Nov;291(2):648-54. To Reference
Ref 30Bioorg Med Chem Lett. 2002 Aug 19;12(16):2225-8.Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. To Reference
Ref 31Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies. J Med Chem. 2000 Feb 10;43(3):351-60. To Reference
Ref 32Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9. To Reference
Ref 33RTI-76, an irreversible inhibitor of dopamine transporter binding, increases locomotor activity in the rat at high doses. Brain Res. 2001 Apr 6;897(1-2):157-63. To Reference



 

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