| + |
FGFR3 | up-regulates activity 
phosphorylation
|
GLO1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276181 |
Tyr136 |
GIAVPDVySACKRFE |
in vitro |
|
| pmid |
sentence |
| 34838714 |
We show that Glo1 activity is promoted by phosphorylation on Tyrosine 136 via multiple kinases. Glo1 Y136 is phosphorylated by multiple different kinases including all members of the Src family. Depletion of multiple different kinases led to a partial reduction in Glo1(Y136) phosphorylation. These included members of the Src family (Src, Yes1, FGR, and the related Abl1), and of the FAK, EPHA, FGFR, and VEGFR families (Figure 2B), suggesting phosphorylation of Glo1 on Y136 by multiple different kinases. In vitro kinase assays revealed that all the members of the Src family, as well as Epha5 and VEGFR3, can efficiently phosphorylate recombinant Glo1 on Y136 (Figure 2C–D). |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
FGFR3 | down-regulates activity 
phosphorylation
|
CILK1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277436 |
Tyr15 |
RQLGDGTyGSVLLGR |
in vitro |
|
| pmid |
sentence |
| 30782830 |
FGF signaling partially abolished ICK's kinase activity, through FGFR-mediated ICK phosphorylation at conserved residue Tyr15, which interfered with optimal ATP binding. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
FGFR3 | down-regulates quantity by destabilization
phosphorylation
|
TET2 |
0.253 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277535 |
Tyr1902 |
TRISLVFyQHKSMNE |
Homo sapiens |
HEp-2 Cell |
| pmid |
sentence |
| 33097695 |
FGFR3∆7-9, but not wild-type FGFR3, directly interacts with TET2 and phosphorylates TET2 at Y1902 site, leading to the ubiquitination and proteasome-mediated degradation of TET2. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR3 |
phosphorylation
|
PTEN |
0.437 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191797 |
Tyr240 |
RREDKFMyFEFPQPL |
Homo sapiens |
Glioblastoma Cell |
| pmid |
sentence |
| 22891331 |
Fgfrs phosphorylate pten at tyrosine 240 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR3 | up-regulates activity
phosphorylation
|
FGFR3 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106726 |
Tyr577 |
RRPPGLDySFDTCKP |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3 the absence of y577 (3y-577f) or y760 (3y-760f) resulted in a modest decrease in activity. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106730 |
Tyr647 |
RDVHNLDyYKKTTNG |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3 the two tyrosine residues in the YYKK Motif of the activation loop of fgfrs are required for kinase activity of fgfr1 and fgfr3. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106734 |
Tyr648 |
DVHNLDYyKKTTNGR |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3the two tyrosine residues in the YYKK Motif of the activation loop of fgfrs are required for kinase activity of fgfr1 and fgfr3. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106738 |
Tyr724 |
ANCTHDLyMIMRECW |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3taken together, these results clearly implicate y724 in the activation of stat proteins by constitutively activated mutants of fgfr3 and suggest that both y724 and y760 are required for maximal stat activation. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106742 |
Tyr760 |
TVTSTDEyLDLSAPF |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3taken together, these results clearly implicate y724 in the activation of stat proteins by constitutively activated mutants of fgfr3 and suggest that both y724 and y760 are required for maximal stat activation. |
|
| Publications: |
5 |
Organism: |
Homo Sapiens |
| + |
FGFR3 | up-regulates activity
phosphorylation
|
STAT1 |
0.657 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251138 |
Tyr701 |
DGPKGTGyIKTELIS |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 10918587 |
Activation of Stat1 and Stat3 by FGFR derivatives. Lysates of 293T cells transfected as indicated were analysed by Western blotting using Phospho-Stat1 (Y701) antisera (top) or Stat1 antisera (bottom). (b) The same lysates in (a) were re-examined for phosphorylated Stat3 by Western blotting with Phospho-Stat3 (Y705) (top). all three FGFR family members examined here are able to lead to Stat activation. Expression of the 'TDII-like' derivatives of FGFR1, FGFR3, and FGFR4, as well as myrR1-WT, led to phosphorylation of both Stat1 and Stat3. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR3 | up-regulates activity
phosphorylation
|
STAT3 |
0.615 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251139 |
Tyr705 |
DPGSAAPyLKTKFIC |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 10918587 |
Activation of Stat1 and Stat3 by FGFR derivatives. Lysates of 293T cells transfected as indicated were analysed by Western blotting using Phospho-Stat1 (Y701) antisera (top) or Stat1 antisera (bottom). (b) The same lysates in (a) were re-examined for phosphorylated Stat3 by Western blotting with Phospho-Stat3 (Y705) (top). all three FGFR family members examined here are able to lead to Stat activation. Expression of the 'TDII-like' derivatives of FGFR1, FGFR3, and FGFR4, as well as myrR1-WT, led to phosphorylation of both Stat1 and Stat3. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR3 | down-regulates activity
phosphorylation
|
FGFR3 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-106746 |
Tyr770 |
LSAPFEQySPGGQDT |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 11294897 |
Ligand stimulation leads to autophosphorylation of fgfr3these results suggest that y770 may negatively regulate the activation of pi 3-kinase by constitutively activated fgfr3 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
Brivanib alaninate | down-regulates
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190723 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| 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 acid | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259705 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
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-258081 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
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 |
| + |
FGF2 | up-regulates
binding
|
FGFR3 |
0.813 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-134788 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15780951 |
Fgf-2 and fgf-9 increased expression of other osteogenic factors bmp-2 and tgf-beta1, and endogenous fgf/fgfr signaling is a positive upstream regulator of the bmp-2 gene in calvarial osteoblasts. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-195588 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 22298955 |
Fgf-2 and fgf-9 increased expression of other osteogenic factors bmp-2 and tgf-beta1, and endogenous fgf/fgfr signaling is a positive upstream regulator of the bmp-2 gene in calvarial osteoblasts. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
FGF1 | up-regulates
binding
|
FGFR3 |
0.793 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-195585 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 22298955 |
Reports also show that fgf/fgfr3 signals mediate some of the effects of tgf-beta on embryonic bone formation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
4-amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydrobenzimidazol-2-ylidene]-2-quinolinone | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258105 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
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 |
| + |
PD173074 | down-regulates
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205728 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
nintedanib | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257798 |
|
|
in vitro |
|
| pmid |
sentence |
| 18559524 |
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 |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259279 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
BGJ-398 | down-regulates
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190269 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
pazopanib hydrochloride | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259165 |
|
|
in vitro |
|
| pmid |
sentence |
| 17620431 |
Pazopanib inhibition of a number of kinases outside of the VEGFR family was also determined. These included Abl1; Akt3; activin-like kinase 6; cyclin-dependent kinase 1/cyclin A; cyclin-dependent kinase 2/cyclin A; c-fms; c-Kit; epidermal growth factor receptor; ErbB2; ErbB4; EphB4; focal adhesion kinase; FGF receptors (FGFR) 1, 2, and 3; Flt-3; glycogen synthase kinase 3; insulin-like growth factor type I receptor; insulin receptor; interleukin-2–inducible T-cell kinase; c-jun NH2-terminal kinases 1, 2, and 3; lymphocyte-specific protein tyrosine kinase (murine); Met; p38α; PDGFRα and PDGFRβ; protein kinase C-β1 and -β2; polo-like kinases 1 and 3; Ret; Src; Syk; Tie-2; and Wee1. All assays were conducted using purified, recombinantly expressed catalytic domains of the kinases. |
|
| Publications: |
1 |
Organism: |
In Vitro |
3.0
FGFR3
- 
- 