PDZ binding kinase

Target id: 2140

Nomenclature: PDZ binding kinase

Abbreviated Name: PBK

Family: TOPK family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 322 8p21.2 PBK PDZ binding kinase
Mouse - 330 14 D1 Pbk PDZ binding kinase
Rat - 337 15p12 Pbk PDZ binding kinase
Previous and Unofficial Names
Spermatogenesis-related protein kinase
T-LAK cell-originated protein kinase
SPK
TOPK
cancer/testis antigen 84 ( CT84 )
T–lymphokine-activated killer cell–originated protein kinase
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.12.2
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
OTS964 Hs Inhibition 7.55 pIC50 2
pIC50 7.55 (IC50 2.8x10-8 M) [2]
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/PBK(TOPK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 2.7
staurosporine Hs Inhibitor Inhibition 27.8
JAK inhibitor I Hs Inhibitor Inhibition 39.1
SB 218078 Hs Inhibitor Inhibition 39.9
Y27632 Hs Inhibitor Inhibition 56.7
GSK-3beta inhibitor II Hs Inhibitor Inhibition 62.7
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 64.5
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 66.2
Syk inhibitor II Hs Inhibitor Inhibition 66.4
PKR inhibitor Hs Inhibitor Inhibition 67.4
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Matsuo Y, Park JH, Miyamoto T, Yamamoto S, Hisada S, Alachkar H, Nakamura Y. (2014) TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med6 (259): 259ra145. [PMID:25338756]

How to cite this page

TOPK family: PDZ binding kinase. Last modified on 27/10/2014. Accessed on 21/12/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2140.