Target Information

Target General Infomation
Target ID
T09909
Former ID
TTDS00525
Target Name
Type-2 angiotensin II receptor
Gene Name
AGTR2
Synonyms
AT2; Angiotensin II receptor 2; AGTR2
Target Type
Successful
Disease Hypertension [ICD9: 401; ICD10: I10-I16]
Postherpetic neuralgia [ICD9: 53.19; ICD10: B02.2, G44.847, G53.0]
Function
Receptor for angiotensin II. Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation.
BioChemical Class
GPCR rhodopsin
Target Validation
T09909
UniProt ID
P50052
Sequence
MKGNSTLATTSKNITSGLHFGLVNISGNNESTLNCSQKPSDKHLDAIPILYYIIFVIGFL
VNIVVVTLFCCQKGPKKVSSIYIFNLAVADLLLLATLPLWATYYSYRYDWLFGPVMCKVF
GSFLTLNMFASIFFITCMSVDRYQSVIYPFLSQRRNPWQASYIVPLVWCMACLSSLPTFY
FRDVRTIEYLGVNACIMAFPPEKYAQWSAGIALMKNILGFIIPLIFIATCYFGIRKHLLK
TNSYGKNRITRDQVLKMAAAVVLAFIICWLPFHVLTFLDALAWMGVINSCEVIAVIDLAL
PFAILLGFTNSCVNPFLYCFVGNRFQQKLRSVFRVPITWLQGKRESMSCRKSSSLREMET
FVS
Drugs and Mode of Action
Drug(s) SARALASIN Drug Info Approved Hypertension [541252], [551871]
EMA-401 Drug Info Phase 2 Postherpetic neuralgia [525181], [543095]
Hypertension NCE Drug Info Phase 1 Hypertension [551509]
MP-157 Drug Info Phase 1 Hypertension [549248]
Fonsartan Drug Info Discontinued in Phase 2 Hypertension [545886]
L-158282 Drug Info Discontinued in Phase 2 Discovery agent [545352]
TAK-591 Drug Info Discontinued in Phase 1 Hypertension [548747]
L-158809 Drug Info Terminated Hypertension [544926]
L-159689 Drug Info Terminated Hypertension [545497]
L-162234 Drug Info Terminated Discovery agent [545499]
PD-123319 Drug Info Terminated Discovery agent [541248], [544968]
SC-50560 Drug Info Terminated Discovery agent [545548]
SC-51895 Drug Info Terminated Discovery agent [545549]
Inhibitor ANGIOTENSIN II Drug Info [551256]
L-158282 Drug Info [551261]
L-158809 Drug Info [551261]
L-159093 Drug Info [533939]
L-159689 Drug Info [551315]
L-162234 Drug Info [525772]
L-162313 Drug Info [530937]
Macrocyclic Quinazolinone analogue Drug Info [551315]
PD-123319 Drug Info [530232]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ala Drug Info [530232]
Sar-Arg-Val-Tyr-Ile-His-Pro-Ile Drug Info [530232]
Sar-Arg-Val-Tyr-Ile-His-Pro-Phe-OH Drug Info [530734]
SARALASIN Drug Info [529789]
SC-50560 Drug Info [551257]
SC-51895 Drug Info [551257]
SC-52892 Drug Info [551257]
SC-55634 Drug Info [551257]
Agonist angiotensin III Drug Info [543785]
CGP42112 Drug Info [531462]
compound 21 Drug Info [531967]
MP-157 Drug Info [549742]
[125I]CGP42112 Drug Info [528955]
Antagonist EMA-401 Drug Info [551699]
PD123177 Drug Info [532113]
TAK-591 Drug Info [551717]
Modulator Fonsartan Drug Info [534815]
Hypertension NCE Drug Info [543785]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Adrenergic signaling in cardiomyocytes
Renin-angiotensin system
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways ACE Inhibitor Pathway
GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 525181ClinicalTrials.gov (NCT02435199) Clinical Trial Designed to Determine the Safety and Efficacy of EMA401 in Patients With Painful Diabetic Neuropathy. U.S. National Institutes of Health.
Ref 541248(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: 597).
Ref 541252(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: 598).
Ref 543095(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: 8374).
Ref 544926Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001562)
Ref 544968Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001732)
Ref 545352Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002983)
Ref 545497Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003495)
Ref 545499Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003503)
Ref 545548Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003674)
Ref 545549Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003677)
Ref 545886Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005209)
Ref 548747Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028308)
Ref 549248Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034178)
Ref 551509Biopharmaceutical Research Companies Are Developing More Than 430 Medicines for Top Chronic Diseases Affecting Older Americans. Pharmaceutical Research and Manufacturers of America report. 2014.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525772J Med Chem. 2000 May 18;43(10):1993-2006.Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.
Ref 528955Radioiodinated CGP 42112A: a novel high affinity and highly selective ligand for the characterization of angiotensin AT2 receptors. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1365-71.
Ref 529789J 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.
Ref 530232J 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.
Ref 530734J Med Chem. 1991 Apr;34(4):1514-7.1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists.
Ref 530937Bioorg 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.
Ref 531462Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin Sci (Lond). 2011 Oct;121(7):297-303.
Ref 531967Compound 21 induces vasorelaxation via an endothelium- and angiotensin II type 2 receptor-independent mechanism. Hypertension. 2012 Sep;60(3):722-9.
Ref 532113Two distinct angiotensin II receptor binding sites in rat adrenal revealed by new selective nonpeptide ligands. Mol Pharmacol. 1990 Mar;37(3):347-51.
Ref 533939J Med Chem. 1993 Oct 15;36(21):3207-10.A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.
Ref 534815Role of the angiotensin II AT2-subtype receptors in the blood pressure-lowering effect of losartan in salt-restricted rats. J Hypertens. 1998 Dec;16(12 Pt 2):2039-43.
Ref 543785(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. (Target id: 35).
Ref 549742As drug target reemerges, the question is to block or stimulate it. Nature Medicine. Spoonful of Medicine. 05 Feb 2014. Cassandra Willyard
Ref 551256The preparation of (perfluoroalkyl)imidazoles as nonpeptide angiotensin II receptor antagonists, Bioorg. Med. Chem. Lett. 3(5):895-898 (1993).
Ref 551257N1-sterically hindered 2H-imidazol-2-one angiotensin II receptor antagonists: The conversion of surmountable antagonists to insurmountable antagonists, Bioorg. Med. Chem. Lett. 3(6):1055-1060 (1993).
Ref 551261Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors, Bioorg. Med. Chem. Lett. 4(1):189-194 (1994).
Ref 551315The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists, Bioorg. Med. Chem. Lett. 6(8):923-928 (1996).
Ref 551699Clinical pipeline report, company report or official report of Spinifex.
Ref 551717Clinical pipeline report, company report or official report of Takeda (2009).

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