EC Number   |
Application |
Reference |
|---|
   2.7.10.1 | analysis |
large-scale proteomic approach to identify over 200 substrates of the receptor tyrosine kinases kinase family in cancer cell lines driven by the c-Met, epidermal growth factor receptor, or platelet-derived growth factor receptor alpha receptor tyrosine kinases. For a subset of proteins with RxRxxS/T sites, phosphorylation is decreased by receptor tyrosine kinase inhibitors as well as by inhibitors of the PI3K, mTOR, and MAPK pathways. Phosphorylation of the protein chaperone small glutamine-rich tetratricopeptide repeat-containing protein alpha at Ser305 is essential for PDGFRalpha stabilization and cell survival in PDGFRalpha-dependent cancer cells |
723768 |
| 2.7.10.1 | analysis |
proximity ligation assay-based methodology for in situ visualization and quantification of ligand-dependent EGFR receptor dimerization in intact cells. Using the approach combined with a universally applicable epitope tagging strategy, EGFR dimers can be detect in cells transiently co-expressing FLAG-tagged and MYC-tagged human EGFRs. Data strongly suggest that the method can be used to detect ligand-dependent EGFR dimerization, and the signal is generated in a protein interaction-based manner |
721883 |
| 2.7.10.1 | diagnostics |
analysis of in situ ERBB signaling networks in conjunction with ex vivo drug response profiling and biochemical dissection of adaptive RTK activities may serve as a valid diagnostic approach to identify tumors sensitive to ERBB network inhibition |
761882 |
| 2.7.10.1 | drug development |
aminoquinazoline pyridones are potent, selective, and orally efficacious c-Kit inhibitors for the treatment of fibrotic diseases. Compounds show greater than 200fold selectivity against KDR, p38, Lck, and Src |
-, 693545 |
| 2.7.10.1 | drug development |
genetically altered RTKs and their coupled PI3K/Akt and MAPK pathways may play an extensive role in the tumorigenesis and aggressiveness of anaplastic thyroid cancer, thus specific genotype-based targeting at these signaling pathways may be an effective therapeutic strategy for anaplastic thyroid cancer |
693346 |
| 2.7.10.1 | drug development |
inhibitors of tyrosine kinases, offer the opportunity to reverse chemotherapy resistance and enhance response in patients with localized and advanced breast cancer |
690447 |
| 2.7.10.1 | drug development |
N-alkyl and N-unsubstituted naphthamides are potent and selective inhibitors of KDR |
693539 |
| 2.7.10.1 | drug development |
new series of C-5 substituted indazolylaminoquinazolines as potent ErbB2 kinase inhibitors |
691267 |
| 2.7.10.1 | drug development |
new substance class (4-(indole-3-yl)quinazolines) for the treatment of EGFR-dependent tumors, showing strong fluorescences. No connection between cytotoxicity and EGFR-TK inhibition |
692173 |
| 2.7.10.1 | drug development |
novel series of 4-aminopyrimidine-5-carbaldehyde oximes that are potent and selective inhibitors of both EGFR and ErbB-2 tyrosine kinases |
691283 |
