Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T07400
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| Former ID |
TTDR00745
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| Target Name |
Advanced glycosylation end product-specific receptor
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| Gene Name |
AGER
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| Synonyms |
RAGE; RAGESEC; Receptor foradvanced glycosylation end products; AGER
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| Target Type |
Clinical Trial
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| Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
| Dementia [ICD9: 290-294; ICD10: F01-F07] | |||||
| Diabetic kidney disease; Diabetic nephropathy [ICD9:250.4; ICD10: E11.22, E11.21] | |||||
| Hypotension [ICD9: 458, 796.3; ICD10: I95] | |||||
| Function |
Mediates interactions of advanced glycosylation end products (age). These are nonenzymatically glycosylated proteins which accumulate in vascular tissue in aging and at an accelerated rate in diabetes. Receptor for amyloid beta peptide.
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| BioChemical Class |
Immunoglobulin
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| UniProt ID | |||||
| Sequence |
MAAGTAVGAWVLVLSLWGAVVGAQNITARIGEPLVLKCKGAPKKPPQRLEWKLNTGRTEA
WKVLSPQGGGPWDSVARVLPNGSLFLPAVGIQDEGIFRCQAMNRNGKETKSNYRVRVYQI PGKPEIVDSASELTAGVPNKVGTCVSEGSYPAGTLSWHLDGKPLVPNEKGVSVKEQTRRH PETGLFTLQSELMVTPARGGDPRPTFSCSFSPGLPRHRALRTAPIQPRVWEPVPLEEVQL VVEPEGGAVAPGGTVTLTCEVPAQPSPQIHWMKDGVPLPLPPSPVLILPEIGPQDQGTYS CVATHSSHGPQESRAVSISIIEPGEEGPTAGSVGGSGLGTLALALGILGGLGTAALLIGV ILWQRRQRRGEERKAPENQEEEEERAELNQSEEPEAGESSTGGP |
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| Drugs and Mode of Action | |||||
| Drug(s) | PF-4494700 | Drug Info | Phase 3 | Dementia | [1], [2] |
| Pyridoxamine | Drug Info | Phase 3 | Diabetic kidney disease; Diabetic nephropathy | [3] | |
| Alagebrium chloride | Drug Info | Phase 2/3 | Hypotension | [4] | |
| TTP-448 | Drug Info | Phase 2 | Alzheimer disease | [5] | |
| TTP-4000 | Drug Info | Phase 1 | Alzheimer disease | [6] | |
| Breaker | Alagebrium chloride | Drug Info | [7], [8] | ||
| Modulator | DBT-066 | Drug Info | [9] | ||
| TTP-448 | Drug Info | [10] | |||
| Antagonist | PF-4494700 | Drug Info | [10] | ||
| Inhibitor | Pyridoxamine | Drug Info | [11], [12] | ||
| TTP-4000 | Drug Info | [13] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| Pathway Interaction Database | amb2 Integrin signaling | ||||
| Reactome | RIP-mediated NFkB activation via ZBP1 | ||||
| DEx/H-box helicases activate type I IFN and inflammatory cytokines production | |||||
| TAK1 activates NFkB by phosphorylation and activation of IKKs complex | |||||
| Advanced glycosylation endproduct receptor signaling | |||||
| TRAF6 mediated NF-kB activation | |||||
| WikiPathways | NRF2 pathway | ||||
| Nuclear Receptors Meta-Pathway | |||||
| Cytosolic sensors of pathogen-associated DNA | |||||
| TAK1 activates NFkB by phosphorylation and activation of IKKs complex | |||||
| AGE/RAGE pathway | |||||
| RIG-I/MDA5 mediated induction of IFN-alpha/beta pathways | |||||
| Advanced glycosylation endproduct receptor signaling | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT02080364) Evaluation of the Efficacy and Safety of Azeliragon (TTP488) in Patients With Mild Alzheimer's Disease. U.S. National Institutes of Health. | ||||
| REF 2 | (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: 8317). | ||||
| REF 3 | ClinicalTrials.gov (NCT02156843) Pyridorin in Diabetic Nephropathy. U.S. National Institutes of Health. | ||||
| REF 4 | ClinicalTrials.gov (NCT01417663) Effects of Exercise Training and AGE-crosslink Breaker on Cardiovascular Structure and Function. U.S. National Institutes of Health. | ||||
| REF 5 | Biopharmaceutical Research Companies are Developing Nearly 100 Medicines for Alzheimer's Disease and Other Dementias. Pharmaceutical Research and Manufacturers of America report. 2012. | ||||
| REF 6 | ClinicalTrials.gov (NCT01548430) A Safety Study of TTP4000 in Subjects With Alzheimer's Disease. U.S. National Institutes of Health. | ||||
| REF 7 | Effect of the age cross-link breaker alagebrium on anterior segment physiology, morphology, and ocular age and rage. Trans Am Ophthalmol Soc. 2009 Dec;107:146-58. | ||||
| REF 8 | Alagebrium reduces glomerular fibrogenesis and inflammation beyond preventing RAGE activation in diabetic apolipoprotein E knockout mice. Diabetes. 2012 Aug;61(8):2105-13. | ||||
| REF 9 | (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: 2843). | ||||
| REF 10 | Receptor for advanced glycation endproduct modulators: a new therapeutic target in Alzheimer's disease. Expert Opin Investig Drugs. 2015 Mar;24(3):393-9. | ||||
| REF 11 | The AGE inhibitor pyridoxamine inhibits development of retinopathy in experimental diabetes. Diabetes. 2002 Sep;51(9):2826-32. | ||||
| REF 12 | Pyridoxamine, an inhibitor of advanced glycation end product (AGE) formation ameliorates insulin resistance in obese, type 2 diabetic mice. Protein Pept Lett. 2010 Sep;17(9):1177-81. | ||||
| REF 13 | Receptor for advanced glycation end products: its role in Alzheimer's disease and other neurological diseases. Future Neurol. 2009; 4(2): 167-177. | ||||
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