Target Information

Target General Infomation
Target ID
T74456
Former ID
TTDS00267
Target Name
Type-1 angiotensin II receptor
Gene Name
AGTR1
Synonyms
AT1; AT1AR; Angiotensin 1 receptor; Angiotensin II receptor 1; AGTR1
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Hypertension [ICD9: 401; ICD10: I10-I16]
Heart failure [ICD9: 428; ICD10: I50]
Hypotension [ICD9: 458, 796.3; ICD10: I95]
High blood pressure [ICD9: 401; ICD10: I10-I16]
Metabolic syndrome x [ICD9: 277.7; ICD10: E88.81]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Restenosis [ICD10: I51.89]
Unspecified [ICD code not available]
Function
Receptor for angiotensin II.Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T74456
UniProt ID
P30556
Sequence
MILNSSTEDGIKRIQDDCPKAGRHNYIFVMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLK
TVASVFLLNLALADLCFLLTLPLWAVYTAMEYRWPFGNYLCKIASASVSFNLYASVFLLT
CLSIDRYLAIVHPMKSRLRRTMLVAKVTCIIIWLLAGLASLPAIIHRNVFFIENTNITVC
AFHYESQNSTLPIGLGLTKNILGFLFPFLIILTSYTLIWKALKKAYEIQKNKPRNDDIFK
IIMAIVLFFFFSWIPHQIFTFLDVLIQLGIIRDCRIADIVDTAMPITICIAYFNNCLNPL
FYGFLGKKFKRYFLQLLKYIPPKAKSHSNLSTKMSTLSYRPSDNVSSSTKKPAPCFEVE
Drugs and Mode of Action
Drug(s) Azilsartan Drug Info Approved Hypertension [1], [2]
Candesartan Drug Info Approved Hypertension [3], [4]
Eprosartan Drug Info Approved Hypertension [3], [5]
Forasartan Drug Info Approved Hypertension [6], [7]
Irbesartan Drug Info Approved Hypertension [8], [9]
Losartan Drug Info Approved Hypertension [8], [10]
Micardis telmisartan Drug Info Approved Hypertension [11]
Olmesartan medoxomil Drug Info Approved High blood pressure [12]
Saprisartan Drug Info Approved Hypertension [13], [14]
SARALASIN Drug Info Approved Hypertension [15], [16]
Saralasin Acetate Drug Info Approved Hypertension [16]
Tasosartan Drug Info Approved Hypertension [3], [17]
Telmisartan Drug Info Approved Hypertension [3], [18]
Valsartan Drug Info Approved Hypertension [3], [19]
Pratosartan Drug Info Phase 3 Hypertension [20]
S-474474 Drug Info Phase 3 Metabolic syndrome x [21]
TAK-491 Drug Info Phase 3 Hypertension [22]
CL-329167 Drug Info Phase 2 Hypertension [23]
sparsentan Drug Info Phase 2 Myocardial infarction [24]
TRV027 Drug Info Phase 2 Heart failure [25]
YM-358 Drug Info Phase 2 Hypertension [26]
KRH-594 Drug Info Discontinued in Phase 2 Hypertension [27]
MILFASARTAN Drug Info Discontinued in Phase 2 Hypertension [28]
RIPISARTAN Drug Info Discontinued in Phase 2 Hypertension [29]
Zolasartan Drug Info Discontinued in Phase 2 Hypotension [30]
TAK-591 Drug Info Discontinued in Phase 1 Hypertension [31]
UR-7198 Drug Info Discontinued in Phase 1 Hypertension [32]
CR-3834 Drug Info Terminated Hypertension [33]
HELENALIN Drug Info Terminated Discovery agent [34]
L-159689 Drug Info Terminated Hypertension [35]
RS-66252 Drug Info Terminated Alzheimer disease [36]
UP-275-22 Drug Info Terminated Hypertension [37]
XR-510 Drug Info Terminated Hypertension [38]
Antagonist (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n Drug Info [39]
4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone Drug Info [40]
4-[(diphenylmethyl)amino]-2-phenylquinazoline Drug Info [41]
5-butyl-methyl immidazole carboxylate 30 Drug Info [42]
5-oxo-1-2-4-oxadiazol biphenyl Drug Info [43]
Candesartan Drug Info [44], [45]
CL-329167 Drug Info [46], [16]
CR-3834 Drug Info [47]
Eprosartan Drug Info [48]
EXP3174 Drug Info [49]
Forasartan Drug Info [50], [6]
GBR-12935 Drug Info [51]
Irbesartan Drug Info [52]
KRH-594 Drug Info [53]
Losartan Drug Info [54], [55], [52]
LY301875 Drug Info [56]
LY303336 Drug Info [56]
Micardis telmisartan Drug Info [57]
MILFASARTAN Drug Info [58], [16]
N,N`-bis-alkyl butylimmidazole 12b Drug Info [59]
Olmesartan medoxomil Drug Info [60]
Pratosartan Drug Info [61]
RIPISARTAN Drug Info [62], [16]
Saprisartan Drug Info [13]
sparsentan Drug Info [63]
TAK-591 Drug Info [64]
Tasosartan Drug Info [65]
Telmisartan Drug Info [66]
TRV027 Drug Info [67]
UR-7198 Drug Info [68]
Valsartan Drug Info [55], [52]
YM-358 Drug Info [69], [16]
[125I]EXP985 Drug Info [70]
[3H]A81988 Drug Info [71]
[3H]candesartan Drug Info [72]
[3H]eprosartan Drug Info [73]
[3H]irbesartan Drug Info [74]
[3H]L158809 Drug Info [75]
[3H]losartan Drug Info [76]
[3H]valsartan Drug Info [77]
Inhibitor 4-(2-Butyl-benzoimidazol-1-ylmethyl)-phenol Drug Info [78]
ANGIOTENSIN II Drug Info [79]
Carboxylic Acid Metabolite (E-3174) Drug Info [80]
CV-11194 Drug Info [81]
GNF-PF-2307 Drug Info [82]
GNF-PF-2812 Drug Info [82]
GNF-PF-3832 Drug Info [82]
HELENALIN Drug Info [82]
L-159093 Drug Info [63]
L-159689 Drug Info [63]
L-162313 Drug Info [83]
L-162782 Drug Info [83]
SARALASIN Drug Info [84]
[Bpa1]AngII Drug Info [79]
[Sar1,Bpa2]AngII Drug Info [79]
[Sar1,Bpa3]AngII Drug Info [79]
[Sar1,Bpa8]AngII Drug Info [79]
[Sar1,Tdf2]AngII Drug Info [79]
[Sar1,Tdf3]AngII Drug Info [79]
[Sar1,Tdf8]AngII Drug Info [79]
[Tdf1]AngII Drug Info [79]
Agonist angiotensin III Drug Info [85]
L-163,101 Drug Info [86]
Zolasartan Drug Info [87]
Modulator Azilsartan Drug Info [88]
CGP-49870 Drug Info
RS-66252 Drug Info [89]
Saralasin Acetate Drug Info [90]
TAK-491 Drug Info [88]
UP-275-22 Drug Info [85]
XR-510 Drug Info [91]
Blocker S-474474 Drug Info [21]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
Adrenergic signaling in cardiomyocytes
Vascular smooth muscle contraction
Renin-angiotensin system
Renin secretion
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Angiotensin II-stimulated signaling through G proteins and beta-arrestin
Pathway Interaction Database Arf6 trafficking events
Arf6 signaling events
Angiopoietin receptor Tie2-mediated signaling
PathWhiz Pathway Angiotensin Metabolism
Muscle/Heart Contraction
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways ACE Inhibitor Pathway
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Allograft Rejection
GPCR ligand binding
GPCR downstream signaling
References
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REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 588).
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REF 67First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers. J Clin Pharmacol. 2013 Sep;53(9):892-9.
REF 68Pharmacologic profile of UR-7247, an orally active angiotensin II AT1 receptor antagonist, in healthy volunteers. p6. J Cardiovasc Pharmacol. 2000 Mar;35(3):383-9.
REF 69Effects of YM358, an angiotensin II type 1 (AT1) receptor antagonist, and enalapril on blood pressure and vasoconstriction in two renal hypertension models. Biol Pharm Bull. 2000 Feb;23(2):174-81.
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REF 72Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells. Eur J Pharmacol. 1999 Feb 19;367(2-3):413-22.
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