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Reversible protein phosphorylation mediated by kinases and phosphatases plays an important role in cellular function regulations such as cell proliferation, apoptosis, subcellular translocation, inflammation and metabolism. The human kinase group includes 518 known protein kinases and about 20 lipid kinases. As we know that most of the kinase inhibitors target highly conserved ATP-binding sites, and highly selective drugs are pursued in terms of their superior safety profile compared to lower selectivity inhibitors, where lower selectivity drugs have off-target kinases inhibition, inhibit cancer cell growth by relieving multiple kinase-dependent pathways, and induce toxic side effects in clinic.
The kinase activity evaluation is critical for biochemical research, clinical diagnosis and drug targeted therapy for serious diseases. The study of a rapid, simple, sensitive and specific method for detecting kinase activity has a wide application prospect, and high-throughput screening (HTS) was used widely developing highly selective inhibitors, and so kinase profiling has become an important standard for the kinase inhibitors evaluation.
The ICE Bioscience has developed a kinase profiling platform based on HTRF and ADP-GLO methods to facilitate the development of new drugs, such as CDK kinase panel (16 types) and TK kinase panel (76 types), 60 mini kinase panel, 207 wild-type kinase panel and 310 kinase panel as shown in the appendix below.
Welcome any further discussion on the assay details and validation data.
Keywords： kinase profiling; Off-target effect; High throughput screening;
Pictures：
Figure 1 FDA-approved kinase inhibitors mapped onto the human kinome
References：
1. Attwood Misty M,Fabbro Doriano,Sokolov Aleksandr V et al. Trends in kinase drug discovery: targets, indications and inhibitor design.[J] .Nat Rev Drug Discov, 2021, 20: 839-861.
Validation data:
Appendix：
CDK family kinase panel (16 kinases) | |||
CDK1/CycA2 | CDK3/CycE1 | CDK6/CycD1 | CDK12/CycK |
CDK1/CycE1 | CDK4/CycD3 | CDK6/CycD3 | CDK13/CycK |
CDK2/CycA2 | CDK5/p25NCK | CDK7/CycH/MAT1 | CDK16/CycY |
CDK2/CycE1 | CDK5/p35NCK | CDK9/CycT1 | CDK18/CycY |
TK kinase panel list | |||||||
ALK | EGFR | EPHA8 | FGFR3 | HER2 | KIT | RET | TRKC |
ABL1 | DDR1 | EPHB1 | FGFR4 | Her4 | LCK | RON | TXK |
ABL2 | DDR2 | EPHB2 | FGR | IGF1R | LYNa | ROS1 | TYK2 |
ACK | EPHA1 | EPHB3 | FLT1 | INSR | LYNb | SRC | TYRO3 |
AXL | EPHA2 | EPHB4 | FLT3 | IRR | MER | SRM | YES |
BMX | EPHA3 | FAK | FLT4 | ITK | MET | SYK | ZAP70 |
BRK | EPHA4 | FER | FRK | JAK1 | MUSK | TEC | |
BTK | EPHA5 | FES | FYN [isoform a] | JAK2 | PDGFRα | TIE2 | |
CSF1R | EPHA6 | FGFR1 | FYN [isoform b] | JAK3 | PDGFRβ | TRKA | |
CSK | EPHA7 | FGFR2 | HCK | KDR | PYK2 | TRKB | |
Mini kinase panel (60 kinases) | |||
ABL1 | CK1γ2 | IGF1R | PDGFRα |
AKT1 | CK1γ3 | IKK-alpha | PIM1 |
ALK 4 | CK2a1 | ITK | PKACα |
AMPKα1/β1/γ1 | CLK1 | JAK3 | PKCα |
AurB | DAPK1 | JNK1 | PKD2 |
AXL | DCAMKL2 | KDR | PLK1 |
BRAF | DYRK1B | LCK | PLK2 |
BRSK2 | EGFR | MAP2K1 | ROCK1 |
CDK1/CycE1 | EPHB4 | MAPKAPK2 | RSK1 |
CDK18 <31 2022-08 最新动态
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