Target Information
Target General Infomation | |||||
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Target ID |
T09909
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Former ID |
TTDS00525
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Target Name |
Type-2 angiotensin II receptor
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Gene Name |
AGTR2
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Synonyms |
AT2; Angiotensin II receptor 2; AGTR2
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Target Type |
Successful
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T09909
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UniProt ID | |||||
Sequence |
MKGNSTLATTSKNITSGLHFGLVNISGNNESTLNCSQKPSDKHLDAIPILYYIIFVIGFL
VNIVVVTLFCCQKGPKKVSSIYIFNLAVADLLLLATLPLWATYYSYRYDWLFGPVMCKVF GSFLTLNMFASIFFITCMSVDRYQSVIYPFLSQRRNPWQASYIVPLVWCMACLSSLPTFY FRDVRTIEYLGVNACIMAFPPEKYAQWSAGIALMKNILGFIIPLIFIATCYFGIRKHLLK TNSYGKNRITRDQVLKMAAAVVLAFIICWLPFHVLTFLDALAWMGVINSCEVIAVIDLAL PFAILLGFTNSCVNPFLYCFVGNRFQQKLRSVFRVPITWLQGKRESMSCRKSSSLREMET FVS |
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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 525181 | ClinicalTrials.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 544926 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001562) | ||||
Ref 544968 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001732) | ||||
Ref 545352 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002983) | ||||
Ref 545497 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003495) | ||||
Ref 545499 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003503) | ||||
Ref 545548 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003674) | ||||
Ref 545549 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003677) | ||||
Ref 545886 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005209) | ||||
Ref 548747 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028308) | ||||
Ref 549248 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034178) | ||||
Ref 525772 | J Med Chem. 2000 May 18;43(10):1993-2006.Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity. | ||||
Ref 528955 | Radioiodinated 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 529789 | J 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 530232 | J 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 530734 | J Med Chem. 1991 Apr;34(4):1514-7.1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists. | ||||
Ref 530937 | Bioorg 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 531462 | Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin Sci (Lond). 2011 Oct;121(7):297-303. | ||||
Ref 531967 | Compound 21 induces vasorelaxation via an endothelium- and angiotensin II type 2 receptor-independent mechanism. Hypertension. 2012 Sep;60(3):722-9. | ||||
Ref 532113 | Two distinct angiotensin II receptor binding sites in rat adrenal revealed by new selective nonpeptide ligands. Mol Pharmacol. 1990 Mar;37(3):347-51. | ||||
Ref 533939 | J Med Chem. 1993 Oct 15;36(21):3207-10.A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor. | ||||
Ref 534815 | Role 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 549742 | As drug target reemerges, the question is to block or stimulate it. Nature Medicine. Spoonful of Medicine. 05 Feb 2014. Cassandra Willyard | ||||
Ref 551256 | The preparation of (perfluoroalkyl)imidazoles as nonpeptide angiotensin II receptor antagonists, Bioorg. Med. Chem. Lett. 3(5):895-898 (1993). | ||||
Ref 551257 | N1-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 551261 | Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors, Bioorg. Med. Chem. Lett. 4(1):189-194 (1994). |
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