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激酶谱筛选|激酶谱|药物靶点筛选|爱思益普

时间:2022-08-31 15:54:44 阅读:111

  激酶在细胞增殖、分化和代谢等生理过程的调控中担任着重要的角色。众多的人类疾病与激酶的活性异常有着直接或者间接的关系。人类激酶组包括518种已知的蛋白激酶和大约20种脂质激酶。到目前为止,大多数蛋白激酶抑制剂药物都针对高度保守的ATP结合位点。虽然一些低选择性的抑制剂已被证明通过解除多种激酶依赖途径有效抑制癌细胞生长,但高选择性药物由于其能减少脱靶效应带来的毒副作用,有着更为优越的安全性。

  对激酶活性的分析检测对于生化研究、临床诊断及对重大疾病的药物靶向治疗等都具有重要意义。研究快速、简单、灵敏度高和特异性好的检测激酶活性的新方法具有广泛的应用前景。而在寻找高选择性抑制剂的过程中,针对激酶谱的高通量筛选(HTS)成为一个重要的鉴定方法,激酶谱筛选是激酶抑制剂选择性评价的重要标准。

  爱思益普团队已开发出基于HTRF及ADP-Glo方法的激酶谱检测平台,助力新药研发。 目前可以提供的激酶谱筛选服务包括CDK激酶谱(16种)、酪氨酸激酶谱(TK共76种)、60 mini 激酶谱、207野生型激酶谱、310激酶谱。详细靶点列表可见附录。

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1  FDA批准的人类激酶组激酶抑制剂

  参考文献:

  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.

  内部验证数据

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附录:

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

HIPK1

p70S6K

TRKB

CK1α

HPK1

PAK2

TSSK1

 

207 kinase panel list

ABL1

DDR2

IRR

PAK5

TXK

ABL2

DYRK1A

ITK

PDGFRα

TYK2

ACK

DYRK1B

JAK1

PDGFRβ

TTK

AKT1

DYRK2

JAK2

PIK3CA

TYRO3

AKT2

DYRK3

JAK3

PIM1

YES

AKT3

DYRK4

JNK1

PIM2

YSK1

ALK

EGFR

JNK2

PIM3

ZAP70

ALK 4

EPHA1

JNK3

PKD1


AMPKα1/β1/γ1

EPHA2

KDR

PKD2


AurA

EPHA3

KHS

PKD3


AurB

EPHA4

KIT

PKR


AurC

EPHA5

LCK

PKACα


AXL

EPHA6

LYNa

PLK1


BLK

EPHA7

LYNb

PLK3


BMX

EPHA8

MAP2K1

PYK2


BRAF

EPHB1

MAP3K2

QIK


BRK

EPHB2

MAP3K3

RET


BRSK1 

EPHB3

MAP3K19

ROCK 1


BRSK2

EPHB4

MAP4K2

ROCK 2


BTK

Erk1

MAPKAPK2

RON


CDK1/CycB1

Erk5

MAPKAPK5

ROS1


CDK1/CycA2

FAK

MARK1 

RSK1


CDK1/CycE1

FER

MARK2 

RSK2


CDK16/CycY

FES

MARK3 

RSK3


CDK18/CycY

FGFR1

MARK4 

RSK4


CDK2/CycA2

FGFR2

MER

SGK


CDK2/CycE1

FGFR3

MET

SGK2


CDK3/CycE1

FGFR4

MINK

SGK3


CDK5/p25NCK

FGR

MLK1

SIK


CDK5/p35NCK

FLT1

MLK2

SLK


CDK7/CycH/MAT1

FLT3

MLK3

SRC


CDK9/CycT1

FLT4

MRCKα

SRM


CHK1

FMS

MRCKβ

LOK


CHK2

FRK

MUSK

MST3


CK1α

FYN [isoform a]

NEK1

MST2


CK1γ1

FYN [isoform b]

NEK2

MST1


CK1γ2

GLK

NEK9

SYK


CK1γ3

GSK3α

NIM1K 

TAOK1


CK1δ

GSK3β

NuaK1

TAOK2


CK1ε

HCK

NuaK2 

TAOK3


CK2α1/β

HER2

OSR1

TBK1


CK2α2/β

Her4

p38α

TEC


CLK1

HGK

p38β

TGFβR1


CLK3

HIPK1

p38γ

TGFβR2


CLK4

HIPK2

p38δ

TIE2


CSK

HIPK3

p70S6K

TNIK


DAPK1

HIPK4

PAK1

TRKA


DCAMKL1

HPK1

PAK2

TRKB


DCAMKL2

IGF1R

PAK3

TRKC


DDR1

INSR

PAK4

TSSK1


 

310 kinase panel list

ABL1

CK1γ2

EPHB4

HPK1

MLK3

PRKCG

TTBK1

ABL2

CK1γ3

Erk1

IGF1R

MNK1

PYK2

TTBK2

ACK

CK1δ

Erk5

IKKα

MNK2

QIK

TTK

AKT1

CK1ε

Erk7

IKKβ

MRCKα

RET

TXK

AKT2

CK2α1/β

FAK

IKKε

MRCKβ

RET E762Q

TYK2

AKT3

CK2α2/β

FER

INSR

MSK1

RET G691S

TYRO3

ALK

CLK1

FES

IRR

MSK2

RET G810C

WNK4

ALK 4

CLK2

FGFR1

ITK

MST1

RET G810R

YES

AMPKα1/β1/γ1

CLK3

FGFR1 V561M

JAK1

MST2

RET G810S

YSK1

AurA

CLK4

FGFR1 W666R

JAK2

MST3

RET M918T

ZAP70

AurB

CRIK

FGFR2

JAK3

MUSK

RET S891A


AurC

CSK

FGFR2 C491A

JNK1

NDR1

RET S904A


AXL

DAPK1

FGFR2 C491F

JNK2

NDR2

RET S904F


BARK1

DCAMKL1

FGFR2 C491S

JNK3

NEK1

RET V804L


BARK2  

DCAMKL2

FGFR2 E565G

KDR

NEK2

RET V804M


BLK

DDR1

FGFR2 K526E

KHS

NEK3

RET Y806H


BMPR2

DDR2

FGFR2 K659N

KIT

NEK4

RIPK2


BMX

DMPK1

FGFR2 N549H

KIT T670I

NEK9

RIPK3


BRAF

DMPK2

FGFR2 R612T

KIT V559D

NIM1K 

ROCK 1


BRK

DYRK1A

FGFR2 V564F

LATS1

NuaK1

ROCK 2


BRSK1 

DYRK1B

FGFR3

LATS2

NuaK2 

RON


BRSK2

DYRK2

FGFR3 K650E

LCK

OSR1

ROS1


BTK

DYRK3

FGFR4

LIMK1

p38α

RSK1


BUB1/BUB3

DYRK4

FGFR4 N535K

LOK

p38β

RSK2


CaMK1α

EGFR

FGFR4 V550E

LYNa

p38γ

RSK3


CaMK1β

EGFR A763_Y764insFQEA

FGFR4 V550L

LYNb

p38δ

RSK4


CaMK1δ

EGFR C797S

FGFR4 V550M

MAP2K1

p70S6K

SGK


CaMK2α

EGFR d746-750

FGR

MAP2K2

PAK1

SGK2


CaMK2β

EGFR D746-750 T790M

FLT1

MAP3K19

PAK2

SGK3


CaMK2γ

EGFR d746-750 T790M C797S

FLT3

MAP3K2

PAK3

SIK


CaMK2δ

EGFR D770_N771insNPG

FLT3 D835Y

MAP3K3

PAK4

SLK


CDK1/CycA2

EGFR L858R

FLT3 ITD

MAP3K5

PAK5

SRC


CDK1/CycB1

EGFR L861Q

FLT4

MAP4K2

PAK6

SRM


CDK1/CycE1

EGFR T790M

FMS

MAPKAPK2

PASK

SYK


CDK16/CycY

EGFR T790M C797S

FRK

MAPKAPK3

PDGFRα

TAOK1


CDK18/CycY

EGFR T790M C797S L858R

FYN [isoform a]

MAPKAPK5

PDGFRβ

TAOK2


CDK2/CycA2

EGFR T790M L858R

FYN [isoform b]

MARK1 

PGK

TAOK3


CDK2/CycE1

EGFR V769-D770 insGE

GLK

MARK2 

PHKG1

TBK1


CDK3/CycE1

EML4-ALK

GPRK4

MARK3 

PHKG2

TEC


CDK4/CycD3

EPHA1

GPRK7  

MARK4 

PIK3CA

TGFβR1


CDK5/p25NCK

EPHA2

GSK3α

MER

PIM1

TGFβR1 T204D


CDK5/p35NCK

EPHA3

GSK3β

MET

PIM2

TGFβR2


CDK6/CycD1

EPHA4

HCK

MET D1228H

PIM3

TIE2


CDK6/CycD3

EPHA5

HER2

MET D1228N

PKACα

TNIK


CDK7/CycH/MAT1

EPHA6

Her4

MET Y1230A

PKD1

TRKA


CDK9/CycT1

EPHA7

HGK

MET Y1230C

PKD2

TRKA  G667C


CHK1

EPHA8

HIPK1

MET Y1230D

PKD3

TRKA G595R


CHK2

EPHB1

HIPK2

MINK

PKR

TRKB


CK1α

EPHB2

HIPK3

MLK1

PLK1

TRKC


CK1γ1

EPHB3

HIPK4

MLK2

PLK3

TSSK1


 


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