kinase panel|kinase panel screening|fp binding assay-自主发布-资讯-生物在线

kinase panel|kinase panel screening|fp binding assay

作者:北京爱思益普生物科技股份有限公司 2022-09-05T13:26 (访问量:3780)

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

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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:

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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

Erk2

MET

SGK

CDK2/CycE1

FGFR1

NEK1

SRC

CDK5/p35NCK

GSK3β

NEK2

SYK

CHK1

HGK

p38α

TIE2

CHK2

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