Target Information

Target General Infomation
Target ID
T47101
Former ID
TTDC00024
Target Name
Basic fibroblast growth factor receptor 1
Gene Name
FGFR1
Synonyms
CD331 antigen; FGFR-1; Fms-like tyrosine kinase 2; bFGF-R; c-fgr; FGFR1
Target Type
Clinical Trial
Disease Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Alzheimer disease [ICD9: 331; ICD10: G30]
Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Dermatological disease [ICD10: L00-L99]
Endometrial cancer [ICD9: 182; ICD10: C54.1]
Idiopathic pulmonary fibrosis; Non-small cell lung cancer [ICD9:516.3; ICD10: J84.1, C33-C34]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Ovarian cancer [ICD9: 183; ICD10: C56]
Peripheral arterial occlusive disease [ICD10: I73.9]
Retinoblastoma [ICD10: C69.2]
Severe coronary heart disease [ICD9: 414; ICD10: I25.1]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Unspecified [ICD code not available]
BioChemical Class
Kinase
Target Validation
T47101
UniProt ID
P11362
EC Number
EC 2.7.10.1
Sequence
MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD
VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD
ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS
SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN
HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI
GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE
ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS
IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL
GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK
HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL
VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG
RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD
KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF
PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
Drugs and Mode of Action
Drug(s) Nintedanib Drug Info Approved Idiopathic pulmonary fibrosis [1]
E-3810 Drug Info Phase 3 Solid tumours [2], [3]
Nintedanib Drug Info Phase 3 Non-small cell lung cancer [4], [5], [6]
AZD4547 Drug Info Phase 2/3 Solid tumours [7], [8]
AM-001 Drug Info Phase 2 Dermatological disease [9]
BGJ398 Drug Info Phase 2 Cancer [10], [11]
FGF-1 Drug Info Phase 2 Severe coronary heart disease [12]
FP-1039 Drug Info Phase 2 Endometrial cancer [13]
Nintedanib Drug Info Phase 2 Ovarian cancer [14], [6]
JNJ-42756493 Drug Info Phase 1/2 Lymphoma [15]
MK-2461 Drug Info Phase 1/2 Alzheimer disease [16]
ARQ-087 Drug Info Phase 1 Cancer [17]
KW-2449 Drug Info Phase 1 Acute myeloid leukemia [18], [19]
SU-6668 Drug Info Phase 1 Advanced solid tumor [20], [21]
Sulfatinib Drug Info Phase 1 Cancer [22]
BMS-695735 Drug Info Preclinical Solid tumours [23]
PD-0183812 Drug Info Terminated Retinoblastoma [24]
Inhibitor 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info [25]
3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine Drug Info [26]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info [27]
AAL-993 Drug Info [28]
ACTB-1003 Drug Info [29]
ARQ-087 Drug Info [29]
BMS-695735 Drug Info [30]
compound 2c Drug Info [31]
compound 7r Drug Info [32]
compound 8h Drug Info [33]
E-3810 Drug Info [34]
MK-2461 Drug Info [16]
NP-506 Drug Info [35]
PD-0166326 Drug Info [36]
PD-0173952 Drug Info [36]
PD-0173955 Drug Info [36]
PD-0173956 Drug Info [36]
PD-0173958 Drug Info [36]
PD-0179483 Drug Info [36]
PD-0180970 Drug Info [36]
PD-0183812 Drug Info [37]
Ro-4396686 Drug Info [38]
SEMAXINIB Drug Info [28]
SU-6668 Drug Info [39], [40]
Sulfatinib Drug Info [41]
Modulator 3052230 Drug Info
AZD4547 Drug Info [42]
BGJ398 Drug Info [43]
JNJ-42756493 Drug Info [29]
Nintedanib Drug Info [44]
Antagonist AM-001 Drug Info [45]
FP-1039 Drug Info [46]
Binder FGF-1 Drug Info [47]
Agonist SAR-106881 Drug Info [29]
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
PI3K-Akt signaling pathway
Adherens junction
Signaling pathways regulating pluripotency of stem cells
Regulation of actin cytoskeleton
Pathways in cancer
Proteoglycans in cancer
Prostate cancer
Melanoma
Central carbon metabolism in cancer
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Angiogenesis
FGF signaling pathway
Pathway Interaction Database Glypican 1 network
Syndecan-4-mediated signaling events
N-cadherin signaling events
FGF signaling pathway
WikiPathways Regulation of Actin Cytoskeleton
Endochondral Ossification
MAPK Signaling Pathway
Mesodermal Commitment Pathway
Induction (Part 1 of 3)
Integrated Pancreatic Cancer Pathway
Signaling Pathways in Glioblastoma
Neural Crest Differentiation
Signaling by FGFR
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 2ClinicalTrials.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 3(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 4ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health.
REF 5ClinicalTrials.gov (NCT02231164) LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research. U.S. National Institutes of Health.
REF 6(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: 5936).
REF 7ClinicalTrials.gov (NCT02154490) Lung-MAP: S1400 Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IIIB-IV Squamous Cell Lung Cancer. U.S. National Institutes of Health.
REF 8(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: 7707).
REF 9ClinicalTrials.gov (NCT01938599) Study Comparing AM001 Cream to Vehicle in the Treatment of Plaque Psoriasis. U.S. National Institutes of Health.
REF 10ClinicalTrials.gov (NCT02160041) BGJ398 for Patients With Tumors With FGFR Genetic Alterations. U.S. National Institutes of Health.
REF 11(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: 7877).
REF 12(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: 4923).
REF 13ClinicalTrials.gov (NCT01244438) Study of FP-1039 in Subjects With Endometrial Cancers. U.S. National Institutes of Health.
REF 14ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health.
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036975)
REF 16MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
REF 17ClinicalTrials.gov (NCT01752920) Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors. U.S. National Institutes of Health.
REF 18KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.
REF 19(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: 5691).
REF 20A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66.
REF 21(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: 7816).
REF 22ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022289)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014130)
REF 25Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases.
REF 26The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 27J Med Chem. 2009 Jan 22;52(2):278-92.Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
REF 28J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.
REF 29(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: 1808).
REF 30J Med Chem. 2008 Oct 9;51(19):5897-900. Epub 2008 Sep 3.Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
REF 31Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett. 2012 Jul 26;3(9):705-9.
REF 32Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold. Org Biomol Chem. 2015 Jul 28;13(28):7643-54.
REF 33The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
REF 34E-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 35Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50. Epub 2008 Dec 10.5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
REF 36Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors.
REF 37J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
REF 38Bioorg 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 39Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6.
REF 40A 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 41Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
REF 42AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
REF 43Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
REF 442014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
REF 46FGF1-gold nanoparticle conjugates targeting FGFR efficiently decrease cell viability upon NIR irradiation. Int J Nanomedicine. 2012; 7: 5915-5927.
REF 47Marimastat as maintenance therapy for patients with advanced gastric cancer: a randomised trial. Br J Cancer. 2002 Jun 17;86(12):1864-70.

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