Target Information
Target General Infomation | |||||
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Target ID |
T58454
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Former ID |
TTDS00171
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Target Name |
Fibroblast growth factor receptor 2
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Gene Name |
FGFR2
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Synonyms |
FGF-2 receptor; FGFR-2; Keratinocyte growth factor receptor 2; FGFR2
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Target Type |
Successful
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Chronic HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Oral mucositis [ICD9: 528; ICD10: K12.3] | |||||
Periodontitis [ICD9: 523.5; ICD10: K05.4] | |||||
Retinoblastoma [ICD10: C69.2] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptor for acidic and basicfibroblast growth factors.
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BioChemical Class |
Kinase
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Target Validation |
T58454
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MVSWGRFICLVVVTMATLSLARPSFSLVEDTTLEPEEPPTKYQISQPEVYVAAPGESLEV
RCLLKDAAVISWTKDGVHLGPNNRTVLIGEYLQIKGATPRDSGLYACTASRTVDSETWYF MVNVTDAISSGDDEDDTDGAEDFVSENSNNKRAPYWTNTEKMEKRLHAVPAANTVKFRCP AGGNPMPTMRWLKNGKEFKQEHRIGGYKVRNQHWSLIMESVVPSDKGNYTCVVENEYGSI NHTYHLDVVERSPHRPILQAGLPANASTVVGGDVEFVCKVYSDAQPHIQWIKHVEKNGSK YGPDGLPYLKVLKAAGVNTTDKEIEVLYIRNVTFEDAGEYTCLAGNSIGISFHSAWLTVL PAPGREKEITASPDYLEIAIYCIGVFLIACMVVTVILCRMKNTTKKPDFSSQPAVHKLTK RIPLRRQVTVSAESSSSMNSNTPLVRITTRLSSTADTPMLAGVSEYELPEDPKWEFPRDK LTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKM IGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTF KDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKT TNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGH RMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEEYLDLSQPLEQYS PSYPDTRSSCSSGDDSVFSPDPMPYEPCLPQYPHINGSVKT |
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Drugs and Mode of Action | |||||
Drug(s) | Interferon Alfa-2a, Recombinant | Drug Info | Approved | Chronic HCV infection | [536361] |
Palifermin | Drug Info | Approved | Oral mucositis | [536838], [541990] | |
E-3810 | Drug Info | Phase 3 | Solid tumours | [524749], [542632] | |
Trafermin | Drug Info | Phase 3 | Periodontitis | [536297] | |
LY2874455 | Drug Info | Phase 2 | Cancer | [523190], [542973] | |
AEE-788 | Drug Info | Phase 1/2 | Solid tumours | [521635], [542626] | |
MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [530708] | |
BAY1179470 | Drug Info | Phase 1 | Cancer | [524332] | |
PD-0183812 | Drug Info | Terminated | Retinoblastoma | [547217] | |
Inhibitor | ACTB-1003 | Drug Info | [543496] | ||
AEE-788 | Drug Info | [536474] | |||
E-3810 | Drug Info | [525382] | |||
MK-2461 | Drug Info | [530708] | |||
PD-0183812 | Drug Info | [525924] | |||
Platelet factor 4 (PF-4) | Drug Info | [535131] | |||
Ro-4396686 | Drug Info | [528018] | |||
TG-100435 | Drug Info | [528527] | |||
Antagonist | BAY1179470 | Drug Info | [550500] | ||
Binder | Interferon alfa (IFN-alpha) | Drug Info | [536555] | ||
Interferon Alfa-2a, Recombinant | Drug Info | [536555] | |||
Palifermin | Drug Info | [537352] | |||
Modulator | LY2874455 | Drug Info | |||
Activator | Trafermin | Drug Info | [536297] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
KEGG Pathway | MAPK signaling pathway | ||||
Ras signaling pathway | |||||
Rap1 signaling pathway | |||||
Endocytosis | |||||
PI3K-Akt signaling pathway | |||||
Signaling pathways regulating pluripotency of stem cells | |||||
Regulation of actin cytoskeleton | |||||
Pathways in cancer | |||||
Prostate cancer | |||||
Central carbon metabolism in cancer | |||||
NetPath Pathway | IL1 Signaling Pathway | ||||
PANTHER Pathway | FGF signaling pathway | ||||
Pathway Interaction Database | FGF signaling pathway | ||||
Reactome | Activated point mutants of FGFR2 | ||||
WikiPathways | Regulation of Actin Cytoskeleton | ||||
Ectoderm Differentiation | |||||
Organogenesis (Part 2 of 3) | |||||
Induction (Part 1 of 3) | |||||
Cardiac Hypertrophic Response | |||||
Signaling Pathways in Glioblastoma | |||||
Neural Crest Differentiation | |||||
Signaling by FGFR | |||||
MicroRNAs in cardiomyocyte hypertrophy | |||||
Angiogenesis | |||||
References | |||||
Ref 521635 | ClinicalTrials.gov (NCT00107237) AEE788 and Everolimus in Treating Patients With Recurrent or Relapsed Glioblastoma Multiforme. U.S. National Institutes of Health. | ||||
Ref 523190 | ClinicalTrials.gov (NCT01212107) A Study of LY2874455 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
Ref 524332 | ClinicalTrials.gov (NCT01881217) First-in-man Dose Escalation Study of BAY1179470 in Patients With Advanced, Refractory Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524749 | ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536838 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | ||||
Ref 541990 | (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: 6954). | ||||
Ref 542626 | (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: 7643). | ||||
Ref 542632 | (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: 7649). | ||||
Ref 525382 | E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. | ||||
Ref 525924 | J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. | ||||
Ref 528018 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. | ||||
Ref 528527 | Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 535131 | A short peptide domain of platelet factor 4 blocks angiogenic key events induced by FGF-2. FASEB J. 2001 Mar;15(3):550-2. Epub 2001 Jan 5. | ||||
Ref 536474 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. | ||||
Ref 536555 | DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. |
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