DGIdb - AGTR1 Gene Record

AGTR1 185 Druggable Genome

Alternate Names:

185
ANGIOTENSIN II RECEPTOR TYPE 1
AGTR1
AG2S
AGTR1B
AT1
AT1AR
AT1B
AT1BR
AT1R
AT2R1
HAT1R
106165
336
ENSG00000144891
OTTHUMG00000159503
P30556
AGTR1_HUMAN
AGTR1A
AT2R1B
Type-1 angiotensin II receptor
Angiotensin II type-1 receptor
34
AT<sub>1</sub> receptor
TYPE-1 ANGIOTENSIN II RECEPTOR (AT1) (AT1AR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30556]
NP_000676
NM_000685
PA43
BE0000062
Angiotensin II receptor type-1
T74456
AT2R1A

Gene Info:

Transmembrane Helix Count	7
Target Subclass	Rhodopsin
Target Subclass	GPCR
Target Main Class	Receptors
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
GuideToPharmacology Gene Category Name	Angiotensin receptors
GuideToPharmacology Gene Category ID	6
Interpro Acc	IPR000276
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Status	Swiss-Prot
Interpro Type	Family
Uniprot Evidence	1: Evidence at protein level
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(11 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Unger, 2001, Pharmacology of AT1-receptor blockers., Blood Press Suppl
Elokdah et al., 2002, Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects., Bioorg. Med. Chem. Lett.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Maillard et al., 2000, Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding., J. Pharmacol. Exp. Ther.
Rocha et al., 2003, Angiotensin AT1 receptor antagonist losartan and the defence reaction in the anaesthetised rat. Effect on the carotid chemoreflex., Exp. Physiol.
Dickstein et al., 1998, Losartan: a selective angiotensin II type 1 (AT1) receptor antagonist for the treatment of heart failure., Expert Opin Investig Drugs
Anand-Srivastava et al., 2003, Angiotensin-II-induced enhanced expression of Gi proteins is attenuated by losartan in A10 vascular smooth muscle cells: role of AT1 receptors., Can. J. Physiol. Pharmacol.
Ismail MA et al., 2006, Design and synthesis of new tetrazolyl- and carboxy-biphenylylmethyl-quinazolin-4-one derivatives as angiotensin II AT1 receptor antagonists., J Med Chem
Sookoian S et al., 2005, A1166C angiotensin II type 1 receptor gene polymorphism may predict hemodynamic response to losartan in patients with cirrhosis and portal hypertension., Am J Gastroenterol
Miller JA et al., 1999, Angiotensin II type 1 receptor gene polymorphism predicts response to losartan and angiotensin II., Kidney Int
Arsenault J et al., 2010, A single-nucleotide polymorphism of alanine to threonine at position 163 of the human angiotensin II type 1 receptor impairs Losartan affinity., Pharmacogenet Genomics
Sardo et al., Effects of AT1 receptor antagonist losartan on sICAM-1 and TNF-alpha levels in uncomplicated hypertensive patients., Angiology
Guan et al., 2004, [The effects of losartan on pulmonary arterial collagen and AT1 in chronic hypoxic rats]., Sichuan Da Xue Xue Bao Yi Xue Ban
Usune et al., 1996, Effects of SC-52458, a new nonpeptide angiotensin II receptor antagonist, on increase in cytoplasmic Ca2+ concentrations and contraction induced by angiotensin II and K(+)-depolarization in guinea-pig taenia coli., Gen. Pharmacol.
Hagmann et al., 1997, SC-52458, an orally active angiotensin II-receptor antagonist: inhibition of blood pressure response to angiotensin II challenges and pharmacokinetics in normal volunteers., J. Cardiovasc. Pharmacol.
Tokunaga et al., 2001, Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia., Jpn. J. Pharmacol.
Wassmann et al., 2001, Inhibition of geranylgeranylation reduces angiotensin II-mediated free radical production in vascular smooth muscle cells: involvement of angiotensin AT1 receptor expression and Rac1 GTPase., Mol. Pharmacol.
Wu, From bedside to bench drug-induced tubulointerstitial disease cyclosporine nephropathy study from models of cultured renal epithelial cells., Chang Gung Med J
van den Meiracker et al., 1995, Hemodynamic and biochemical effects of the AT1 receptor antagonist irbesartan in hypertension., Hypertension
Morsing et al., 1999, Mechanistic differences of various AT1-receptor blockers in isolated vessels of different origin., Hypertension
Adams et al., 2000, Irbesartan: review of pharmacology and comparative properties., Can J Clin Pharmacol
Croom et al., 2004, Irbesartan: a review of its use in hypertension and in the management of diabetic nephropathy., Drugs
Martin et al., 2004, Lesion progression in apoE-deficient mice: implication of chemokines and effect of the AT1 angiotensin II receptor antagonist irbesartan., J. Cardiovasc. Pharmacol.
Croom et al., 2008, Irbesartan: a review of its use in hypertension and diabetic nephropathy., Drugs
Carraway et al., 1999, Comparison of irbesartan with captopril effects on cardiac hypertrophy and gene expression in heart failure-prone male SHHF/Mcc-fa(cp) rats., J. Cardiovasc. Pharmacol.
Hope et al., 1999, Comparison of the effects of AT1 receptor blockade and angiotensin converting enzyme inhibition on atherosclerosis., Am. J. Hypertens.
Dol et al., 2001, Angiotensin AT1 receptor antagonist irbesartan decreases lesion size, chemokine expression, and macrophage accumulation in apolipoprotein E-deficient mice., J. Cardiovasc. Pharmacol.
Waeber et al., 2003, AT1-receptor antagonism in hypertension: what has been learned with irbesartan?, Expert Rev Cardiovasc Ther
Voigt et al., 2007, Hypophagic effect of the angiotensin AT1 receptor antagonist irbesartan in rats., Eur. J. Pharmacol.
Mazzolai et al., 1999, Angiotensin II receptor blockade in normotensive subjects: A direct comparison of three AT1 receptor antagonists., Hypertension
Timmermans, 1999, Pharmacological properties of angiotensin II receptor antagonists., Can J Cardiol
Uemura et al., 2006, Renin-angiotensin system is an important factor in hormone refractory prostate cancer., Prostate
Nap et al., 2003, Pre- and postsynaptic inhibitory potencies of the angiotensin AT1 receptor antagonists eprosartan and candesartan., Eur. J. Pharmacol.
Suzuki et al., 2003, Effects of the AT1-receptor antagonist eprosartan on the progression of left ventricular dysfunction in dogs with heart failure., Br. J. Pharmacol.
Ruilope et al., 2003, Eprosartan for the treatment of hypertension., Expert Opin Pharmacother
Puig et al., 2002, Clinical profile of eprosartan., Cardiovasc Drugs Ther
de la Sierra et al., 2007, Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction., Curr Med Res Opin
Heusser et al., 2003, AT1 antagonism by eprosartan lowers heart rate variability and baroreflex gain., Auton Neurosci
Hedner, 2002, The clinical profile of the angiotensin II receptor blocker eprosartan., J Hypertens Suppl
Murdoch et al., 2001, ADEPT: Addition of the AT1 receptor antagonist eprosartan to ACE inhibitor therapy in chronic heart failure trial: hemodynamic and neurohormonal effects., Am. Heart J.
Gremmler et al., 2000, Improvement of cardiac output in patients with severe heart failure by use of ACE-inhibitors combined with the AT1-antagonist eprosartan., Eur. J. Heart Fail.
Ilson et al., 1998, The effects of eprosartan, an angiotensin II AT1 receptor antagonist, on uric acid excretion in patients with mild to moderate essential hypertension., J Clin Pharmacol
Criscione et al., 1993, Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype., Br. J. Pharmacol.
Shargorodsky et al., 2002, Prolonged treatment with the AT1 receptor blocker, valsartan, increases small and large artery compliance in uncomplicated essential hypertension., Am. J. Hypertens.
de Gasparo et al., 1995, Binding of valsartan to mammalian angiotensin AT1 receptors., Regul. Pept.
Azizi et al., 2004, Pharmacologic demonstration of the synergistic effects of a combination of the renin inhibitor aliskiren and the AT1 receptor antagonist valsartan on the angiotensin II-renin feedback interruption., J. Am. Soc. Nephrol.
Siragy et al., 2002, Differences in AT2 -receptor stimulation between AT1 -receptor blockers valsartan and losartan quantified by renal interstitial fluid cGMP., J. Hypertens.
Kreutz et al., 2006, Pharmacokinetics of olmesartan medoxomil plus hydrochlorothiazide combination in healthy subjects., Clin Drug Investig
Koike et al., 2001, In vitro and in vivo pharmacology of olmesartan medoxomil, an angiotensin II type AT1 receptor antagonist., J Hypertens Suppl
Mire et al., 2005, A review of the structural and functional features of olmesartan medoxomil, an angiotensin receptor blocker., J. Cardiovasc. Pharmacol.
Ochiai et al., 2006, Functional and bioenergetic consequences of AT1 antagonist olmesartan medoxomil in hearts with postinfarction LV remodeling., J. Cardiovasc. Pharmacol.
Warner et al., 2002, Olmesartan medoxomil., Drugs
Rogers et al., 2007, Effect of sex hormones on renal estrogen and angiotensin type 1 receptors in female and male rats., Am. J. Physiol. Regul. Integr. Comp. Physiol.
Volkan-Salanci B et al., 2009, Impact of renin-angiotensin system polymorphisms on renal haemodynamic responsiveness to acute angiotensin-converting enzyme inhibition in type 2 diabetes mellitus., J Renin Angiotensin Aldosterone Syst
Malmqvist et al., 2000, Angiotensin II type 1 (AT1) receptor blockade in hypertensive women: benefits of candesartan cilexetil versus enalapril or hydrochlorothiazide., Am. J. Hypertens.
Meredith, 2007, Candesartan cilexetil--a review of effects on cardiovascular complications in hypertension and chronic heart failure., Curr Med Res Opin
Wada et al., 1996, Comparison of the antihypertensive effects of the new angiotensin II (AT1) receptor antagonist candesartan cilexetil (TCV-116) and the angiotensin converting enzyme inhibitor enalapril in rats., Hypertens. Res.
Engelhorn et al., 2006, Reduction of cerebral infarct size by the AT1-receptor blocker candesartan, the HMG-CoA reductase inhibitor rosuvastatin and their combination. An experimental study in rats., Neurosci. Lett.
Baguet et al., 2009, Candesartan cilexetil in the treatment of chronic heart failure., Vasc Health Risk Manag
Mendis et al., 2009, Candesartan: widening indications for this angiotensin II receptor blocker?, Expert Opin Pharmacother
de Denus S et al., 2008, Effects of AGTR1 A1166C gene polymorphism in patients with heart failure treated with candesartan., Ann Pharmacother
Caballero-George et al., 2003, In vitro effect of sanguinarine alkaloid on binding of [3H]candesartan to the human angiotensin AT1 receptor., Eur. J. Pharmacol.
McInnes et al., 2000, Comparison of the AT1-receptor blocker, candesartan cilexetil, and the ACE inhibitor, lisinopril, in fixed combination with low dose hydrochlorothiazide in hypertensive patients., J Hum Hypertens
Vauquelin et al., 2006, Long-lasting angiotensin type 1 receptor binding and protection by candesartan: comparison with other biphenyl-tetrazole sartans., J Hypertens Suppl
Cervenka et al., 1999, Renal responses of the nonclipped kidney of two-kidney/one-clip Goldblatt hypertensive rats to type 1 angiotensin II receptor blockade with candesartan., J. Am. Soc. Nephrol.
Liakos et al., 1997, ANG II AT1 and AT2 receptors both inhibit bFGF-induced proliferation of bovine adrenocortical cells., Am. J. Physiol.
McClellan et al., 1998, Telmisartan., Drugs
Gohlke et al., 2001, AT1 receptor antagonist telmisartan administered peripherally inhibits central responses to angiotensin II in conscious rats., J. Pharmacol. Exp. Ther.
Yamagishi et al., 2005, Telmisartan is a promising cardiometabolic sartan due to its unique PPAR-gamma-inducing property., Med. Hypotheses
Tagami et al., 2009, A selective peroxisome proliferator-activated receptor-gamma modulator, telmisartan, binds to the receptor in a different fashion from thiazolidinediones., Endocrinology
Sharpe et al., 2001, Telmisartan: a review of its use in hypertension., Drugs
Imayama et al., 2006, Telmisartan downregulates angiotensin II type 1 receptor through activation of peroxisome proliferator-activated receptor gamma., Cardiovasc. Res.
Fujimoto et al., 2004, An angiotensin II AT1 receptor antagonist, telmisartan augments glucose uptake and GLUT4 protein expression in 3T3-L1 adipocytes., FEBS Lett.
Karlberg et al., 1999, Efficacy and safety of telmisartan, a selective AT1 receptor antagonist, compared with enalapril in elderly patients with primary hypertension. TEES Study Group., J. Hypertens.
Balt et al., 2001, Effect of the AT1-receptor antagonists losartan, irbesartan, and telmisartan on angiotensin II-induced facilitation of sympathetic neurotransmission in the rat mesenteric artery., J. Cardiovasc. Pharmacol.
Galzerano et al., 2010, New standards in hypertension and cardiovascular risk management: focus on telmisartan., Vasc Health Risk Manag
Strohmenger et al., 1997, Effects of the AT1-selective angiotensin II antagonist, telmisartan, on hemodynamics and ventricular function after cardiopulmonary resuscitation in pigs., Resuscitation
Yamagishi et al., 2007, Potential utility of telmisartan, an angiotensin II type 1 receptor blocker with peroxisome proliferator-activated receptor-gamma (PPAR-gamma)-modulating activity for the treatment of cardiometabolic disorders., Curr. Mol. Med.
Kurtz, 2008, Beyond the classic angiotensin-receptor-blocker profile., Nat Clin Pract Cardiovasc Med
Tamura et al., 1999, Renin-angiotensin system and fibronectin gene expression in Dahl Iwai salt-sensitive and salt-resistant rats., J. Hypertens.
Bäumer et al., 2001, Reduction of oxidative stress and AT1 receptor expression by the selective oestrogen receptor modulator idoxifene., Br. J. Pharmacol.
Brugts JJ et al., 2010, Tailored therapy of ACE inhibitors in stable coronary artery disease: pharmacogenetic profiling of treatment benefit., Pharmacogenomics
Benetos A et al., 1996, Influence of the angiotensin II type 1 receptor gene polymorphism on the effects of perindopril and nitrendipine on arterial stiffness in hypertensive individuals., Hypertension
Leduc et al., 1995, Involvement of a tyrosine kinase pathway in the growth-promoting effects of angiotensin II on aortic smooth muscle cells., Mol. Pharmacol.
Cheng et al., 1998, Young SHR express increased type 1 angiotensin II receptors in renal proximal tubule., Am. J. Physiol.
Kim JH et al., 2012, Fimasartan, a novel angiotensin II receptor antagonist., Arch Pharm Res

EPROSARTAN AGTR1

Interaction Score: 17.82

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12782193 12540520 12517247 12766389 18093407 11752352 12927226 12184062 11320369 10856732 9602957

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology
FORASARTAN AGTR1

Interaction Score: 8.91

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8981065 9156352 11569611 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank
VALSARTAN AGTR1

Interaction Score: 6.68

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8242249 12460705 8577935 15579516 12023686 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
SAPRISARTAN AGTR1

Interaction Score: 6.68

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10579749 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank
OLMESARTAN AGTR1

Interaction Score: 6.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Direct Interaction? True

Specific Action of the Ligand Antagonist

PMIDs:
17163232 11451212 16220064 11752352 16775509 12076183

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
TASOSARTAN AGTR1

Interaction Score: 5.01

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
11683476 12113820 11752352 11046101

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology
AZILSARTAN AGTR1

Interaction Score: 4.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name azilsartan medoxomil, TAK-491

Novel drug target Established target

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions
TELMISARTAN AGTR1

Interaction Score: 2.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name telmisartan,Micardis, Micardis HCT

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
9878991 11408526 15617852 19147680 11558835 16938288 15498586 10067800 11444497 20448797 9259062 11752352 17691961 18580862

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
FIMASARTAN AGTR1

Interaction Score: 2.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
22864732

Sources:
DrugBank
CANDESARTAN AGTR1

Interaction Score: 2.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10826401 17588300 10968199 16901636 19436650 19563275 11752352 18594050 12504781 10805052 16601569 9892163

Sources:
TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology
LOSARTAN AGTR1

Interaction Score: 2.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12719755 15991937 12710529 16509571 15743363 10594793 20436376 15026875 11752352 15573751

Sources:
TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology
IRBESARTAN AGTR1

Interaction Score: 1.76

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7843749 10373224 10822210 15101793 14716205 18627212 11752352 10069682 10075381 11486244 15030294 17408613 10082498

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
LOSARTAN POTASSIUM AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CL-329167 AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AZILSARTAN MEDOXOMIL AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SARALASIN ACETATE AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
EPROSARTAN MESYLATE AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL347610 AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SPARSENTAN AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions
CHEMBL400912 AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AZILSARTAN KAMEDOXOMIL AGTR1

Interaction Score: 1.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PERINDOPRIL AGTR1

Interaction Score: 0.67

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20712529 8952600

Sources:
PharmGKB
SARALASIN AGTR1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
OLMESARTAN MEDOXOMIL AGTR1

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
IDOXIFENE AGTR1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11588112

Sources:
NCI
PRATOSARTAN AGTR1

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions
CHEMBL1972216 AGTR1

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1445650 AGTR1

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL421088 AGTR1

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYT006-ANGQB AGTR1

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
CHEMBL2094484 AGTR1

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL261693 AGTR1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1390716 AGTR1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CANDESARTAN CILEXETIL AGTR1

Interaction Score: 0.19

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
VOLANESORSEN SODIUM AGTR1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10100098

Sources:
NCI
CHEMBL1492017 AGTR1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NITRENDIPINE AGTR1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8952600

Sources:
PharmGKB
CHEMBL591834 AGTR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ANDROSTANOLONE AGTR1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16990489 16482568

Sources:
NCI
CAPTOPRIL AGTR1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19286758

Sources:
PharmGKB
CHEMBL125044 AGTR1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL586135 AGTR1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL528694 AGTR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HELENALIN AGTR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEVODOPA AGTR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9458818

Sources:
NCI
INDOMETHACIN AGTR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9357777

Sources:
NCI
ATORVASTATIN AGTR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11179461

Sources:
NCI PharmGKB
GENISTEIN AGTR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7476882

Sources:
NCI
CYCLOSPORINE AGTR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17477024

Sources:
NCI
DISULFIRAM AGTR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DEXAMETHASONE AGTR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16482568

Sources:
NCI

Ensembl: ENSG00000144891
- Version: 101_38
Alternate Names:

AGTR1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P30556
- Version: 01-August-2011
Alternate Names:

P30556 Uniprot Accession

185 Entrez Gene Id

AGTR1_HUMAN Uniprot Id

Gene Info:

Transmembrane Helix Count 7

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
HopkinsGroom: P30556
- Version: 11-September-2012
Alternate Names:

TYPE-1 ANGIOTENSIN II RECEPTOR Uniprot Protein Name

185 Entrez Gene Id

AGTR1 Uniprot Gene Name

Gene Info:

Interpro Acc IPR000276

Interpro Short Name 7TM_GPCR_Rhodpsn

Human Readable Name G PROTEIN COUPLED RECEPTOR

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000144891
- Version: 26-July-2011
Alternate Names:

AGTR1 Display Id

ENSG00000144891 Ensembl Gene Id

TYPE-1 ANGIOTENSIN II RECEPTOR (AT1) (AT1AR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30556] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P30556
- Version: January-2014
Alternate Names:

AGTR1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacology: 185
- Version: 29-September-2020
Alternate Names:

336 HUGO Gene ID

336 HUGO Gene Symbol

angiotensin II receptor type 1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Angiotensin receptors

GuideToPharmacology Gene Category ID 6

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: AGTR1

Version: 18-August-2020

Alternate Names:

PA43 PharmGKB ID

Gene Info:

Publications:

de Denus S et al., 2008, Effects of AGTR1 A1166C gene polymorphism in patients with heart failure treated with candesartan., Ann Pharmacother

Bozkurt O et al., 2009, Variation in Renin-Angiotensin system and salt-sensitivity genes and the risk of diabetes mellitus associated with the use of thiazide diuretics., Am J Hypertens

Lee JK et al., 2013, Genetic variation-optimized treatment benefit of angiotensin-converting enzyme inhibitors in patients with stable coronary artery disease: a 12-year follow-up study., Pharmacogenet Genomics

DrugBank: BE0000062

Version: 5.1.7

Alternate Names:

AGTR1 DrugBank Gene Name

P30556 UniProt Accession

185 Entrez Gene Id

Gene Info:

Publications:

Criscione et al., 1993, Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype., Br. J. Pharmacol.

Shargorodsky et al., 2002, Prolonged treatment with the AT1 receptor blocker, valsartan, increases small and large artery compliance in uncomplicated essential hypertension., Am. J. Hypertens.

de Gasparo et al., 1995, Binding of valsartan to mammalian angiotensin AT1 receptors., Regul. Pept.

NCI: AGTR1

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Wu, From bedside to bench drug-induced tubulointerstitial disease cyclosporine nephropathy study from models of cultured renal epithelial cells., Chang Gung Med J

Uemura et al., 2006, Renin-angiotensin system is an important factor in hormone refractory prostate cancer., Prostate

Wassmann et al., 2001, Inhibition of geranylgeranylation reduces angiotensin II-mediated free radical production in vascular smooth muscle cells: involvement of angiotensin AT1 receptor expression and Rac1 GTPase., Mol. Pharmacol.

DTC: AGTR1
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Ismail MA et al., 2006, Design and synthesis of new tetrazolyl- and carboxy-biphenylylmethyl-quinazolin-4-one derivatives as angiotensin II AT1 receptor antagonists., J Med Chem
HingoraniCasas: ENSG00000144891
- Version: 31-May-2017
Alternate Names:

ENSG00000144891 Gene Symbol

AGTR1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: AGTR1A
- Version: chembl_23
Alternate Names:

AGTR1B GENE_SYMBOL

AT2R1 GENE_SYMBOL

AT2R1B GENE_SYMBOL

Gene Info:

Publications:
GO: AGTR1
- Version: 05-September-2020
Alternate Names:

AGTR1A GO Gene Synonym

AGTR1B GO Gene Synonym

AT2R1 GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
dGene: AGTR1
- Version: 27-Jun-2013
Alternate Names:

185 Gene ID

AG2S dGene Synonym

AGTR1A dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Angiotensin II receptor type-1
- Version: 2020.06.01
Alternate Names:

AGTR1 TTD Gene Abbreviation

T74456 TTD Target ID

Gene Info:

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	True

Trial Name	-
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Trial Name	azilsartan medoxomil, TAK-491
Novel drug target	Established target
Mechanism of Interaction	Type-1 angiotensin II receptor antagonist

Trial Name	telmisartan,Micardis, Micardis HCT
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Type-1 angiotensin II receptor antagonist
Direct Interaction	yes

P30556	Uniprot Accession
185	Entrez Gene Id
AGTR1_HUMAN	Uniprot Id

TYPE-1 ANGIOTENSIN II RECEPTOR	Uniprot Protein Name
185	Entrez Gene Id
AGTR1	Uniprot Gene Name

AGTR1	Display Id
ENSG00000144891	Ensembl Gene Id
TYPE-1 ANGIOTENSIN II RECEPTOR (AT1) (AT1AR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30556]	Description

336	HUGO Gene ID
336	HUGO Gene Symbol
angiotensin II receptor type 1	HUGO Gene Name

AGTR1	DrugBank Gene Name
P30556	UniProt Accession
185	Entrez Gene Id

AGTR1A	GO Gene Synonym
AGTR1B	GO Gene Synonym
AT2R1	GO Gene Synonym

AGTR1 Gene Record

AGTR1 185 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 12782193 12540520 12517247 12766389 18093407 11752352 12927226 12184062 11320369 10856732 9602957

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8981065 9156352 11569611 11752352

Sources: TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 8242249 12460705 8577935 15579516 12023686 11752352

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10579749 11752352

Sources: TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Direct Interaction? True Specific Action of the Ligand Antagonist

PMIDs: 17163232 11451212 16220064 11752352 16775509 12076183

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: 11683476 12113820 11752352 11046101

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name azilsartan medoxomil, TAK-491 Novel drug target Established target Mechanism of Interaction Type-1 angiotensin II receptor antagonist

PMIDs: None found

Sources: TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name telmisartan,Micardis, Micardis HCT Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: 9878991 11408526 15617852 19147680 11558835 16938288 15498586 10067800 11444497 20448797 9259062 11752352 17691961 18580862

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 22864732

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 10826401 17588300 10968199 16901636 19436650 19563275 11752352 18594050 12504781 10805052 16601569 9892163

Sources: TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 12719755 15991937 12710529 16509571 15743363 10594793 20436376 15026875 11752352 15573751

Sources: TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 7843749 10373224 10822210 15101793 14716205 18627212 11752352 10069682 10075381 11486244 15030294 17408613 10082498

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Type-1 angiotensin II receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Type-1 angiotensin II receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Type-1 angiotensin II receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12782193 12540520 12517247 12766389 18093407 11752352 12927226 12184062 11320369 10856732 9602957

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8981065 9156352 11569611 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8242249 12460705 8577935 15579516 12023686 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10579749 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Direct Interaction? True

Specific Action of the Ligand Antagonist

PMIDs:
17163232 11451212 16220064 11752352 16775509 12076183

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
11683476 12113820 11752352 11046101

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name azilsartan medoxomil, TAK-491

Novel drug target Established target

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name telmisartan,Micardis, Micardis HCT

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
9878991 11408526 15617852 19147680 11558835 16938288 15498586 10067800 11444497 20448797 9259062 11752352 17691961 18580862

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
22864732

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10826401 17588300 10968199 16901636 19436650 19563275 11752352 18594050 12504781 10805052 16601569 9892163

Sources:
TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12719755 15991937 12710529 16509571 15743363 10594793 20436376 15026875 11752352 15573751

Sources:
TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7843749 10373224 10822210 15101793 14716205 18627212 11752352 10069682 10075381 11486244 15030294 17408613 10082498

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Type-1 angiotensin II receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a