Relation Results

Summary

Name FGFR1
Full Name Fibroblast growth factor receptor 1
Synonyms FGFR-1, Basic fibroblast growth factor receptor 1, BFGFR, bFGF-R-1, Fms-like tyrosine kinase 2, FLT-2, N-sam, Proto-oncogene c-Fgr | BFGFR, CEK, FGFBR, FLG, FLT2, HBGFR
Primary ID P11362
Links - -
Type protein
Relations 59
Pathways Luminal Breast Cancer
Inhibitors sorafenib tosylate; pazopanib; 2-Hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic acid; regorafenib; (2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanol; ponatinib; Brivanib alaninate; BGJ-398; FGFR1; nintedanib; PD173074; orantinib
Function Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic de ...
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Type: Score: Layout: SPV 
0.20.2770.3120.3230.20.3610.3720.20.2580.3520.20.20.20.3160.2950.80.3130.70.9130.8650.20.80.80.80.80.80.80.80.20.80.3130.20.80.8ERK1/2FGFR1MAPK14MAPK1MAPK3PRKCERPS6KA3LDHAAMOTL2BCAR1PDK1SYNCRIPACAT1CTTNPDP1sorafenib tosylateMAP2K1FGF5FGF1FRS2Gbetapazopanib2-Hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic acidregorafenib(2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanolponatinibBrivanib alaninateBGJ-398Non-structural protein 2nintedanibMEK1/2DUSP26PD173074orantinib

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ ERK1/2down-regulates img/direct_inhibition.png phosphorylation FGFR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-244541 Ser777 SMPLDQYsPSFPDTR Homo sapiens
pmid sentence
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling
Publications: 1 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ MAPK14down-regulates img/direct_inhibition.png phosphorylation FGFR1 0.277
Identifier Residue Sequence Organism Cell Line
SIGNOR-166598 Ser777 SMPLDQYsPSFPDTR Homo sapiens
pmid sentence
Fgfr1 translocation requires p38 mapk activation which phosphorylates the c-term tail of fgfr1 on ser777
Publications: 1 Organism: Homo Sapiens
+ MAPK1down-regulates img/direct_inhibition.png phosphorylation FGFR1 0.312
Identifier Residue Sequence Organism Cell Line
SIGNOR-200880 Ser777 SMPLDQYsPSFPDTR Homo sapiens
pmid sentence
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling
Publications: 1 Organism: Homo Sapiens
+ MAPK3down-regulates img/direct_inhibition.png phosphorylation FGFR1 0.323
Identifier Residue Sequence Organism Cell Line
SIGNOR-200884 Ser777 SMPLDQYsPSFPDTR Homo sapiens
pmid sentence
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling
Publications: 1 Organism: Homo Sapiens
+ PRKCEup-regulates img/direct-activation.png phosphorylation FGFR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-201671 Ser779 PLDQYSPsFPDTRSS Homo sapiens Neuron
pmid sentence
Phosphorylation of serine 779 in fibroblast growth factor receptor 1 and 2 by protein kinase c(epsilon) regulates ras/mitogen-activated protein kinase signaling and neuronal differentiationour findings show that in addition to fgfr tyrosine phosphorylation, the phosphorylation of a conserved serine residue, ser(779), can quantitatively control ras/mapk signaling to promote specific cellular responses.
Publications: 1 Organism: Homo Sapiens
+ RPS6KA3down-regulates quantity img/direct_inhibition.png phosphorylation FGFR1 0.361
Identifier Residue Sequence Organism Cell Line
SIGNOR-276599 Ser789 DTRSSTCsSGEDSVF Homo sapiens U2-OS Cell
pmid sentence
 Both in vitro and in vivo experiments confirmed the interaction and we show that phosphorylated RSK2 binds to and phosphorylates serine 789 in the C-terminal tail of FGFR1.prevention of FGFR1 phosphorylation by inhibition of RSK2 activity or mutation of serine 789 to alanine reduced FGFR1 endocytosis and ubiquitination explaining mechanistically the prolonged signaling activity.
Publications: 1 Organism: Homo Sapiens
+ FGFR1up-regulates img/direct-activation.png phosphorylation LDHA 0.372
Identifier Residue Sequence Organism Cell Line
SIGNOR-176730 Tyr10 TLKDQLIyNLLKEEQ Homo sapiens
pmid sentence
We found that the oncogenic receptor tyrosine kinase fgfr1 directly phosphorylates ldh-a. Phosphorylation at y10 and y83 enhances ldh-a activity by enhancing the formation of active, tetrameric ldh-a and the binding of ldh-a substrate nadh, respectively.
Identifier Residue Sequence Organism Cell Line
SIGNOR-176734 Tyr83 KIVSGKDyNVTANSK Homo sapiens
pmid sentence
We found that the oncogenic receptor tyrosine kinase fgfr1 directly phosphorylates ldh-a. Phosphorylation at y10 and y83 enhances ldh-a activity by enhancing the formation of active, tetrameric ldh-a and the binding of ldh-a substrate nadh, respectively.
Publications: 2 Organism: Homo Sapiens
+ FGFR1up-regulates activity img/direct-activation.png phosphorylation AMOTL2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-271869 Tyr107 KGEELPTyEEAKAHS Homo sapiens HEK-293 Cell
pmid sentence
These data support an idea that Amotl2 Tyr-103 can be phosphorylated by FGF receptor tyrosine kinase activity. We then determined whether Amotl2 Tyr-103 is required for its interaction with c-Src. |Amotl2 promotes MAPK/ERK activation via c-Src, which is dependent on phosphorylation of tyrosine residue at position 103 but independent of the C-terminal PDZ-binding domain.
Publications: 1 Organism: Homo Sapiens
+ FGFR1up-regulates img/direct-activation.png phosphorylation BCAR1 0.258
Identifier Residue Sequence Organism Cell Line
SIGNOR-82760 Tyr128 SKAQQGLyQVPGPSP Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98488 Tyr128 SKAQQGLyQVPGPSP Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98492 Tyr249 APGPQDIyDVPPVRG Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98496 Tyr306 PSNHHAVyDVPPSVS Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98500 Tyr327 PLLREETyDVPPAFA Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98569 Tyr410 GVVDSGVyAVPPPAE Homo sapiens
pmid sentence
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas.
Publications: 6 Organism: Homo Sapiens
+ FGFR1up-regulates img/direct-activation.png phosphorylation PDK1 0.352
Identifier Residue Sequence Organism Cell Line
SIGNOR-191719 Tyr136 AEDAKAIyDFTDTVI Homo sapiens
pmid sentence
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-191723 Tyr243 ARRLCDLyYINSPEL Homo sapiens
pmid sentence
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-193454 Tyr244 RRLCDLYyINSPELE Homo sapiens
pmid sentence
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1
Publications: 3 Organism: Homo Sapiens
+ FGFR1up-regulates img/direct-activation.png phosphorylation FGFR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-98622 Tyr154 NRMPVAPyWTSPEKM Homo sapiens
pmid sentence
Tyrosine residues 154 and 307, which are in the extracellular domain of transmembrane receptor isoforms and are in an unusual sequence context for tyrosine phosphorylation, were also phosphorylated.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98626 Tyr280 VEFMCKVySDPQPHI Homo sapiens
pmid sentence
Fgfr signaling is under the control of tyrosine phosphorylation to elicit activation of cellular signaling cascades. Ligand binding induces receptor dimerization and transphosphorylation. Fgfr1 contains eleven tyrosine residues (tyr154, tyr280, tyr307, tyr463, tyr585, tyr605, tyr653, tyr654, tyr730 and tyr766), some of which are directly involved regulating the activity of the receptor and others bind to activate substrates leading to the activation of various transduction pathways.
Identifier Residue Sequence Organism Cell Line
SIGNOR-98630 Tyr307 IGPDNLPyVQILKTA Homo sapiens
pmid sentence
Tyrosine residues 154 and 307, which are in the extracellular domain of transmembrane receptor isoforms and are in an unusual sequence context for tyrosine phosphorylation, were also phosphorylated.
Identifier Residue Sequence Organism Cell Line
SIGNOR-235762 Tyr463 MLAGVSEyELPEDPR Rattus norvegicus Rat-1 Cell
pmid sentence
This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region
Identifier Residue Sequence Organism Cell Line
SIGNOR-236179 Tyr463 MLAGVSEyELPEDPR Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-236183 Tyr583 RRPPGLEyCYNPSHN Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-235906 Tyr583 RRPPGLEyCYNPSHN Rattus norvegicus Rat-1 Cell
pmid sentence
Autophosphorylation of Y653 is followed by the ordered autophosphorylation of several key tyrosine residues within binding sites for the SH2 or PTB domains of signaling proteins that bind to and are phosphorylated by activated FGFR1. This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region
Identifier Residue Sequence Organism Cell Line
SIGNOR-235682 Tyr585 PPGLEYCyNPSHNPE Rattus norvegicus
pmid sentence
Autophosphorylation of Y653 is followed by the ordered autophosphorylation of several key tyrosine residues within binding sites for the SH2 or PTB domains of signaling proteins that bind to and are phosphorylated by activated FGFR1. This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region
Identifier Residue Sequence Organism Cell Line
SIGNOR-236187 Tyr585 PPGLEYCyNPSHNPE Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-98634 Tyr605 KDLVSCAyQVARGME Homo sapiens
pmid sentence
Fgfr signaling is under the control of tyrosine phosphorylation to elicit activation of cellular signaling cascades. Ligand binding induces receptor dimerization and transphosphorylation. Fgfr1 contains eleven tyrosine residues (tyr154, tyr280, tyr307, tyr463, tyr585, tyr605, tyr653, tyr654, tyr730 and tyr766), some of which are directly involved regulating the activity of the receptor and others bind to activate substrates leading to the activation of various transduction pathways.
Identifier Residue Sequence Organism Cell Line
SIGNOR-236195 Tyr653 RDIHHIDyYKKTTNG Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1. We demonstrate that autophosphorylation on tyrosines 653 and 654 is important for activation of tyrosine kinase activity of fgfr1 and is therefore essential for fgfr1-mediated biological responses.
Identifier Residue Sequence Organism Cell Line
SIGNOR-236199 Tyr654 DIHHIDYyKKTTNGR Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1. We demonstrate that autophosphorylation on tyrosines 653 and 654 is important for activation of tyrosine kinase activity of fgfr1 and is therefore essential for fgfr1-mediated biological responses.
Identifier Residue Sequence Organism Cell Line
SIGNOR-235686 Tyr730 SNCTNELyMMMRDCW Rattus norvegicus L-6 Myoblast Cell, PC-12 Cell
pmid sentence
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1
Identifier Residue Sequence Organism Cell Line
SIGNOR-236191 Tyr730 SNCTNELyMMMRDCW Rattus norvegicus
pmid sentence
Furthermore, under conditions in which wild-type or mutant FGFR1 are overexpressed, Y463, Y583, Y585, and Y730 are dispensable for tyrosine phosphorylation of Shc, the mitogen-activated protein kinase (MAPK) response, and stimulation of FGFR1-mediated cell proliferation and differentiation
Identifier Residue Sequence Organism Cell Line
SIGNOR-236203 Tyr766 ALTSNQEyLDLSMPL Rattus norvegicus
pmid sentence
This second-stage autophosphorylation occurs on y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of y463 in the juxtamembrane region, y766 in the c-terminal tail, and y585 in the kinase insert region (1). The third-stage autophosphorylation takes place on the second tyrosine in the activation loop (y654), resulting in an additional 10-fold increase in the intrinsic tyrosine kinase activity of fgfr1.
Publications: 15 Organism: Homo Sapiens, Rattus Norvegicus
Pathways:Luminal Breast Cancer
+ FGFR1down-regulates img/direct_inhibition.png phosphorylation SYNCRIP 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-98704 Tyr373 RVKKLKDyAFIHFDE Homo sapiens
pmid sentence
Novel in vivo tyrosine phosphorylation sites were found in the fgfr-1, phospholipase cgamma, p90 ribosomal s6 kinase, cortactin, and ns-1-associated protein-1. Syncrip, was very recently found to be phosphorylated in response to insulin treatment of 3t3-l1 adipocytes (32). Phosphorylation of syncrip was accommodated by the insulin receptor tyrosine kinase in vitro but was inhibited upon binding of rna. Tyrosine phosphorylation at tyr-373 in the third rna recognition motif domain of nsap1/syncrip can possibly influence its rna binding properties and thus link fgfr-1 signaling to mrna metabolism.
Publications: 1 Organism: Homo Sapiens
+ FGFR1up-regulates activity img/direct-activation.png phosphorylation ACAT1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-264423 Tyr407 HALKQGEyGLASICN Homo sapiens NCI-H1299 Cell
pmid sentence
Treatment with the FGFR1 inhibitor TKI258 in FGFR1-expressing H1299 cells led to decreased Y407 phosphorylation of ACAT1 in the mitochondrial fraction, where both ACAT1 and a fraction of FGFR1 were detected|Inhibition of tetrameric ACAT1 by abolishing Y407 phosphorylation or AH treatment results in decreased ACAT1 activity,
Publications: 1 Organism: Homo Sapiens
+ FGFR1down-regulates img/direct_inhibition.png phosphorylation CTTN 0.316
Identifier Residue Sequence Organism Cell Line
SIGNOR-98618 Tyr446 GTEPEPVySMEAADY Homo sapiens
pmid sentence
Cortactin, which is an actin-binding protein that also plays a role in actin cytoskeleton dynamics (45), was phosphorylated on tyr-446 in our assay (by fgfr1).Phosphorylation of these residues attenuates the f-actin cross-linking activity
Publications: 1 Organism: Homo Sapiens
+ FGFR1down-regulates activity img/direct_inhibition.png phosphorylation PDP1 0.295
Identifier Residue Sequence Organism Cell Line
SIGNOR-276640 Tyr94 SILKANEySFKVPEF Mus musculus NIH-3T3 Cell
pmid sentence
Here we report that phosphorylation at another tyrosine residue, Tyr-94, inhibits PDP1 by reducing the binding ability of PDP1 to lipoic acid, which is covalently attached to the L2 domain of dihydrolipoyl acetyltransferase (E2) to recruit PDP1 to PDC. We found that multiple oncogenic tyrosine kinases directly phosphorylated PDP1 at Tyr-94, and Tyr-94 phosphorylation of PDP1 was common in diverse human cancer cells and primary leukemia cells from patients. 
Publications: 1 Organism: Mus Musculus
+ sorafenib tosylatedown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259221 in vitro
pmid sentence
Further characterization of sorafenib revealed that this molecule was a multikinase inhibitor that targeted the vascular endothelial growth factor receptor family (VEGFR-2 and VEGFR-3) and platelet-derived growth factor receptor family (PDGFR-beta and Kit), which play key roles in tumor progression and angiogenesis. The in vitro and cellular profile of sorafenib is summarized in Table I.
Publications: 1 Organism: In Vitro
+ FGFR1up-regulates img/indirect-activation.png MAP2K1 0.313
Identifier Residue Sequence Organism Cell Line
SIGNOR-218010 Homo sapiens
pmid sentence
 Fibroblast growth factor-2 (FGF-2), in the presence of dexamethasone, isobutylmethylxanthine, and insulin, induces a prolonged activation of the MEK/ERK signaling pathway, which lasts for at least 12 h post-induction, and this activity is less sensitive to the MEK inhibitors
Publications: 1 Organism: Homo Sapiens
+ FGF5up-regulates img/direct-activation.png binding FGFR1 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-38704 Homo sapiens
pmid sentence
Fgf-5 can bind and induce autophosphorylation of human fgf receptors (fgfr) 1 and 2.
Publications: 1 Organism: Homo Sapiens
+ FGF1up-regulates activity img/direct-activation.png binding FGFR1 0.913
Identifier Residue Sequence Organism Cell Line
SIGNOR-236936 Homo sapiens
pmid sentence
Together these data highlight the unique nature of the role of FGF-1 during the earliest stages of adipogenesis and establish a role for FGFR1 in human adipogenesis, identifying FGFR1 as a potential therapeutic target to reduce obesity.
Publications: 1 Organism: Homo Sapiens
Tissue: Adipose Tissue
Pathways:Luminal Breast Cancer
+ FGFR1up-regulates activity img/direct-activation.png phosphorylation FRS2 0.865
Identifier Residue Sequence Organism Cell Line
SIGNOR-236944 Rattus norvegicus L-6 Myoblast Cell
pmid sentence
In this report, we demonstrate that FGF stimulation induces tyrosine phosphorylation of a novel lipid anchored docking protein, termed FRS2, that forms a complex with Grb2/Sos, thus linking FGF-receptor activation to the Ras/MAPK signaling pathway.
Publications: 1 Organism: Rattus Norvegicus
Pathways:Luminal Breast Cancer
+ Gbetadown-regulates img/direct_inhibition.png phosphorylation FGFR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-270013 Homo sapiens
pmid sentence
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling
Publications: 1 Organism: Homo Sapiens
+ pazopanibdown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257735 Homo sapiens HUVEC Cell
pmid sentence
Pyrimidine 13 showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50’s of 84, 74, 140, and 146 nM, respectively.
Publications: 1 Organism: Homo Sapiens
+ 2-Hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic aciddown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258183 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Identifier Residue Sequence Organism Cell Line
SIGNOR-259703 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Publications: 2 Organism: In Vitro
+ regorafenibdown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259177 Homo sapiens
pmid sentence
A novel multi-kinase inhibitor, regorafenib (Figure 1), inhibits vascular endothelial growth factor receptor (VEGFR) 1, VEGFR2, and VEGFR3, that play key roles in angiogenesis, and fibroblast growth factor receptor (FGFR) 1, platelet-derived growth factor receptor-β (PDGFR-β), tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2 (TIE2) and the mutant oncogenic kinase KIT, RET, B-RAF
Publications: 1 Organism: Homo Sapiens
+ FGF1up-regulates img/direct-activation.png binding FGFR1 0.913
Identifier Residue Sequence Organism Cell Line
SIGNOR-83143 Homo sapiens
pmid sentence
Crystal structure of a ternary fgf-fgfr-heparin complex reveals a dual role for heparin in fgfr binding and dimerization.
Publications: 1 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ (2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanoldown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258090 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Publications: 1 Organism: In Vitro
+ ponatinibdown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259277 Homo sapiens
pmid sentence
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family.
Identifier Residue Sequence Organism Cell Line
SIGNOR-259276 Homo sapiens Non-small Cell Lung Cancer Cell
pmid sentence
Ponatinib was able to significantly inhibit the growth of primary lung cancer cultures in vitro. Our data indicate that pharmacological inhibition of FGFR1 kinase activity with ponatinib may be effective for the treatment of lung cancer patients whose tumors overexpress FGFR1.
Publications: 2 Organism: Homo Sapiens
+ Brivanib alaninatedown-regulates img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190717 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ BGJ-398down-regulates img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190263 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ FGFR1down-regulates activity img/direct_inhibition.png chemical inhibition Non-structural protein 2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-260150 Homo sapiens
pmid sentence
Pyrimidine 13 showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50’s of 84, 74, 140, and 146 nM, respectively.
Publications: 1 Organism: Homo Sapiens
+ nintedanibdown-regulates activity img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257804 in vitro
pmid sentence
In this report, we describe the preclinical profile of BIBF 1120, a combined VEGFR, FGFR, and PDGFR inhibitor currently entering phase III clinical studies in non–small cell lung carcinoma and other cancers.
Publications: 1 Organism: In Vitro
+ FGFR1up-regulates img/indirect-activation.png MEK1/2 0.313
Identifier Residue Sequence Organism Cell Line
SIGNOR-244865 Homo sapiens
pmid sentence
Fibroblast growth factor-2 (FGF-2), in the presence of dexamethasone, isobutylmethylxanthine, and insulin, induces a prolonged activation of the MEK/ERK signaling pathway, which lasts for at least 12 h post-induction, and this activity is less sensitive to the MEK inhibitors
Publications: 1 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ DUSP26down-regulates activity img/direct_inhibition.png dephosphorylation FGFR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277104 Homo sapiens
pmid sentence
NEAP and DUSP26 dephosphorylated TrkA and FGFR1 directly.|We found that NEAP, but not its phosphatase-defective mutant, suppressed nerve growth factor (NGF) receptor TrkA and fibroblast growth factor receptor 1 (FGFR1) activation in PC12 cells
Publications: 1 Organism: Homo Sapiens
+ PD173074down-regulates img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-205725 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ orantinibdown-regulates img/direct_inhibition.png chemical inhibition FGFR1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-207435 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
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