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SRSF protein kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 2209

Nomenclature: SRSF protein kinase 2

Abbreviated Name: SRPK2

Family: SRPK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 688 7q22.3 SRPK2 SRSF protein kinase 2
Mouse - 681 5 10.36 cM Srpk2 serine/arginine-rich protein specific kinase 2
Rat - 681 4 q11 Srpk2 SRSF protein kinase 2
Previous and Unofficial Names Click here for help
SFRS protein kinase 2 | SFRSK2 | SR protein kinase 2
Database Links Click here for help
Alphafold P78362 (Hs), O54781 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5668 (Hs)
Ensembl Gene ENSG00000135250 (Hs), ENSMUSG00000062604 (Mm), ENSRNOG00000010601 (Rn)
Entrez Gene 6733 (Hs), 20817 (Mm), 296753 (Rn)
Human Protein Atlas ENSG00000135250 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:6733 (Hs), mmu:20817 (Mm), rno:296753 (Rn)
OMIM 602980 (Hs)
Pharos P78362 (Hs)
RefSeq Nucleotide NM_182691 (Hs), NM_009274 (Mm), NM_001106575 (Rn)
RefSeq Protein NP_872633 (Hs), NP_033300 (Mm), NP_001100045 (Rn)
UniProtKB P78362 (Hs), O54781 (Mm)
Wikipedia SRPK2 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
URMC-099 Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 4
⤷ [4]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
SRPK2 activity is inhibited by >90% in the presence of 1μM URMC-099 [4].
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: SRPK2
Ligand Sp. Type Action Value Parameter
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: SRPK2/SRPK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 17.1 3.0 -3.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 31.0 26.0 1.0
compound 52 [PMID: 9677190] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 37.1 27.0 2.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.9 54.0 12.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.3 34.0 14.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 51.4 36.0 13.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 53.6 32.0 2.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 54.9 53.0 4.0
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 60.6 65.0 27.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 62.0 103.0 89.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

4. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem, 56 (20): 8032-48. [PMID:24044867]

5. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

How to cite this page

SRPK family: SRSF protein kinase 2. Last modified on 25/02/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2209.