Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00525

Target Information
NameType-2 angiotensin II receptor    
Type of targetSuccessful target    
SynonymsAT2    
Angiotensin II receptor 2    
DiseaseHypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[1][2][3]
Drug(s)Candesartan cilexetilApprovedHypertension[4][5]
Candesartan cilexetilMAA and NDA PublishedDiabetic retinopathy[4][5]
AzilsartanPhase IIIHypertension[6]
Azilsartan medoxomilPhase IIIHypertension[6][7]
TAK-491Phase IIIHypertension[8]
PS433540Phase IIbHypertension[8]
TAK-591Phase IHypertension[6]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
Renin-angiotensin system
UniProt IDP50052
FunctionReceptor for angiotensin ii. May have a role in cell morphogenesis and related events in growth and development.    
SequenceMKGNSTLATTSKNITSGLHFGLVNISGNNESTLNCSQKPSDKHLDAIPILYYIIFVIGFL VNIVVVTLFCCQKGPKKVSSIYIFNLAVADLLLLATLPLWATYYSYRYDWLFGPVMCKVF GSFLTLNMFASIFFITCMSVDRYQSVIYPFLSQRRNPWQASYIVPLVWCMACLSSLPTFY FRDVRTIEYLGVNACIMAFPPEKYAQWSAGIALMKNILGFIIPLIFIATCYFGIRKHLLK TNSYGKNRITRDQVLKMAAAVVLAFIICWLPFHVLTFLDALAWMGVINSCEVIAVIDLAL PFAILLGFTNSCVNPFLYCFVGNRFQQKLRSVFRVPITWLQGKRESMSCRKSSSLREMET FVS
Related US Patent6,300,356
6,444,646
6,544,968
6,589,547
6,638,937
6,641,811
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorANGIOTENSIN II[9]
L-158282,   MK-996[10]
L-158809[10]
L-159093[11]
L-159689[12]
L-162234[13]
L-162313[14]
Macrocyclic Quinazolinone analogue[12]
Macrocyclic Quinazolinone analogue[12]
Macrocyclic Quinazolinone analogue[12]
Macrocyclic Quinazolinone analogue[12]
Macrocyclic Quinazolinone analogue[12]
Macrocyclic Quinazolinone analogue[12]
PD-123319[15]
SARALASIN[16]
SC-50560[17]
SC-51895[17]
SC-52458[17]
SC-52892[17]
SC-55634[17]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ala[15]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ile[15]
Sar-Arg-Val-Tyr-Ile-His-Pro-Phe-OH[18]
AntagonistAzilsartan[6]
Azilsartan medoxomil[6][7]
Candesartan cilexetil[4][5]
PS433540[8]
TAK-491[8]
TAK-591[6]
MultitargetTAK-591[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Angiotensin III: a central regulator of vasopressin release and blood pressure. Trends Endocrinol Metab. 2001 May-Jun;12(4):157-62. To Reference
Ref 2Role of the angiotensin AT2 receptor in blood pressure regulation and therapeutic implications. Am J Hypertens. 2001 Jun;14(6 Pt 2):98S-102S. To Reference
Ref 3Angiotensin type 2 receptors: potential importance in the regulation of blood pressure. Curr Opin Nephrol Hypertens. 2001 Jan;10(1):99-103. To Reference
Ref 4AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 5Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. To Reference
Ref 6Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 7Takeda. News for Takeda. 17 Jul 2006. To Reference
Ref 8CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 9Bioorg. Med. Chem. Lett. 3(5):895-898 (1993) To Reference
Ref 10Bioorg. Med. Chem. Lett. 4(1):189-194 (1994) To Reference
Ref 11J Med Chem. 1993 Oct 15;36(21):3207-10.A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor. To Reference
Ref 12Bioorg. Med. Chem. Lett. 6(8):923-928 (1996) To Reference
Ref 13J Med Chem. 2000 May 18;43(10):1993-2006.Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity. To Reference
Ref 14Bioorg Med Chem. 2010 Jun 15;18(12):4570-90. Epub 2010 Apr 9.Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition. To Reference
Ref 15J Med Chem. 1991 Nov;34(11):3248-60.Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. To Reference
Ref 16J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 17Bioorg. Med. Chem. Lett. 3(6):1055-1060 (1993) To Reference
Ref 18J Med Chem. 1991 Apr;34(4):1514-7.1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists. To Reference



 

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