Relation Results

Summary

Name RTKs
Primary ID SIGNOR-PF38
Type protein family
Formed by AATK, ALK, AXL, CSF1R, DDR1, DDR2, EGFR, EPHA1, EPHA2, EPHA3, EPHA4, EPHA5, EPHA6, EPHA7, EPHA8, EPHB1, EPHB2, EPHB3, EPHB4, ERBB2, ERBB3, ERBB4, FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT3, FLT4, IGF1R, INSR, INSRR, KDR, KIT, LMTK2, LTK, MERTK, MET, MST1R, MUSK, NTRK1, NTRK2, NTRK3, PDGFRA, PDGFRB, PTK7, RET, ROR1, ROR2, ROS1, RYK, TEK, TIE1, TYRO3
Relations 11
Pathways Integrin Signaling, Macropinocytosis , PI3K/AKT Signaling, RTKs in cancer

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Type: Score: Layout: SPV 
0.80.20.80.20.80.20.20.20.20.7regorafenibRTKsPI3Ksorafenib tosylateITGB4pazopanib hydrochlorideGFPTK2A6/b4 integrinGRB2GFs

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Relations
Regulator
Mechanism
target
score ℹ
+ regorafenibdown-regulates activity img/direct_inhibition.png chemical inhibition RTKs 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259452 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
Identifier Residue Sequence Organism Cell Line
SIGNOR-259453 Homo sapiens
pmid sentence
In biochemical in vitro or cell-based assays, Regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET,VEGFR 1-3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl at concentrations that can be achieved clinically.
Publications: 2 Organism: Homo Sapiens
+ RTKsup-regulates activity img/direct-activation.png binding PI3K 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-256166 Homo sapiens
pmid sentence
Another phospholipid modifying signaling pathway activated by RTKs is the PI3K pathway. This heterodimeric enzyme comprises two subunits, the p85 regulatory subunit harboring two SH2 domains, and the p110 catalytic subunit. PI3K activation may be achieved by binding of its p85 regulatory subunit to an activated receptor. Alternatively, RTK signaling may activate the small G protein Ras, which in turn recruits PI3K to the plasma membrane and induces a stimulatory conformational change in the lipid kinase
Publications: 1 Organism: Homo Sapiens
Pathways:Integrin Signaling, PI3K/AKT Signaling, RTKs in cancer
+ sorafenib tosylatedown-regulates activity img/direct_inhibition.png chemical inhibition RTKs 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259454 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
+ RTKsup-regulates activity img/direct-activation.png phosphorylation ITGB4 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-259031 Homo sapiens
pmid sentence
The RTKs in turn induce phosphorylation of focal adhesion kinase (FAK) or the signaling domain of the b4 integrin. These elements recruit distinct subsets of signaling enzymes and adaptors, refining the specificity of individual partner RTKs.
Publications: 1 Organism: Homo Sapiens
Pathways:Integrin Signaling
+ pazopanib hydrochloridedown-regulates activity img/direct_inhibition.png chemical inhibition RTKs 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259451 in vitro
pmid sentence
The present study describes an orally bioavailable, ATP-competitive, multitargeted kinase inhibitor, pazopanib (GW786034), and the drug concentration requirement for maximal in vivo activity. Pazopanib is a low nanomolar inhibitor of VEGFR, PDGFR, and c-Kit tyrosine kinases. 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
+ GFup-regulates activity img/direct-activation.png binding RTKs 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-256163 Homo sapiens
pmid sentence
Multiple growth- and differentiation-inducing polypeptide factors bind to and activate transmembrane receptors tyrosine kinases (RTKs), to instigate a plethora of biochemical cascades culminating in regulation of cell fate.
Publications: 1 Organism: Homo Sapiens
Pathways:PI3K/AKT Signaling, RTKs in cancer
+ RTKsup-regulates activity img/direct-activation.png phosphorylation PTK2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-259030 Homo sapiens
pmid sentence
The RTKs in turn induce phosphorylation of focal adhesion kinase (FAK) or the signaling domain of the b4 integrin. These elements recruit distinct subsets of signaling enzymes and adaptors, refining the specificity of individual partner RTKs.
Publications: 1 Organism: Homo Sapiens
Pathways:Integrin Signaling
+ RTKsup-regulates activity img/direct-activation.png phosphorylation A6/b4 integrin 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-259032 Homo sapiens
pmid sentence
The RTKs in turn induce phosphorylation of focal adhesion kinase (FAK) or the signaling domain of the b4 integrin. These elements recruit distinct subsets of signaling enzymes and adaptors, refining the specificity of individual partner RTKs.
Publications: 1 Organism: Homo Sapiens
Pathways:Integrin Signaling
+ RTKsup-regulates activity img/direct-activation.png binding GRB2 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-256167 Homo sapiens
pmid sentence
The adaptor protein Grb2 can bind with activated RTKs through an SH2 domain-phosphotyrosine interaction, while through the SH3 domain (a binding domain specific to proline-rich sequences) Grb2 interacts with the guanine nucleotide exchange factor, Sos.
Publications: 1 Organism: Homo Sapiens
Pathways:Integrin Signaling, PI3K/AKT Signaling, RTKs in cancer
+ GFsup-regulates img/direct-activation.png RTKs 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-256169 Homo sapiens
pmid sentence
Multiple growth- and differentiation-inducing polypeptide factors bind to and activate transmembrane receptors tyrosine kinases (RTKs), to instigate a plethora of biochemical cascades culminating in regulation of cell fate.
Publications: 1 Organism: Homo Sapiens
Pathways:RTKs in cancer
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