Target Information

Target General Infomation
Target ID
T58454
Former ID
TTDS00171
Target Name
Fibroblast growth factor receptor 2
Gene Name
FGFR2
Synonyms
FGF-2 receptor; FGFR-2; Keratinocyte growth factor receptor 2; FGFR2
Target Type
Successful
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.
BioChemical Class
Kinase
Target Validation
T58454
UniProt ID
P21802
EC Number
EC 2.7.10.1
Sequence
MVSWGRFICLVVVTMATLSLARPSFSLVEDTTLEPEEPPTKYQISQPEVYVAAPGESLEV
RCLLKDAAVISWTKDGVHLGPNNRTVLIGEYLQIKGATPRDSGLYACTASRTVDSETWYF
MVNVTDAISSGDDEDDTDGAEDFVSENSNNKRAPYWTNTEKMEKRLHAVPAANTVKFRCP
AGGNPMPTMRWLKNGKEFKQEHRIGGYKVRNQHWSLIMESVVPSDKGNYTCVVENEYGSI
NHTYHLDVVERSPHRPILQAGLPANASTVVGGDVEFVCKVYSDAQPHIQWIKHVEKNGSK
YGPDGLPYLKVLKAAGVNTTDKEIEVLYIRNVTFEDAGEYTCLAGNSIGISFHSAWLTVL
PAPGREKEITASPDYLEIAIYCIGVFLIACMVVTVILCRMKNTTKKPDFSSQPAVHKLTK
RIPLRRQVTVSAESSSSMNSNTPLVRITTRLSSTADTPMLAGVSEYELPEDPKWEFPRDK
LTLGKPLGEGCFGQVVMAEAVGIDKDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKM
IGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTF
KDLVSCTYQLARGMEYLASQKCIHRDLAARNVLVTENNVMKIADFGLARDINNIDYYKKT
TNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGH
RMDKPANCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRILTLTTNEEYLDLSQPLEQYS
PSYPDTRSSCSSGDDSVFSPDPMPYEPCLPQYPHINGSVKT
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)
TEP EXP Info
DRM DRM Info
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 521635ClinicalTrials.gov (NCT00107237) AEE788 and Everolimus in Treating Patients With Recurrent or Relapsed Glioblastoma Multiforme. U.S. National Institutes of Health.
Ref 523190ClinicalTrials.gov (NCT01212107) A Study of LY2874455 in Patients With Advanced Cancer. U.S. National Institutes of Health.
Ref 524332ClinicalTrials.gov (NCT01881217) First-in-man Dose Escalation Study of BAY1179470 in Patients With Advanced, Refractory Solid Tumors. U.S. National Institutes of Health.
Ref 524749ClinicalTrials.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 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536361Natural 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 536838Emerging 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 542973(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: 8104).
Ref 547217Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014130)
Ref 525382E-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 525924J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Ref 528018Bioorg 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 528527Bioorg 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 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 535131A 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 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536474A 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 536555DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29.
Ref 537352Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
Ref 543496(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: 1809).
Ref 550500National Cancer Institute Drug Dictionary (drug id 751593).

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