PAS domain containing serine/threonine kinase | PASK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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PAS domain containing serine/threonine kinase

Target id: 2139

Nomenclature: PAS domain containing serine/threonine kinase

Abbreviated Name: PASK

Family: PASK subfamily

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

   GtoImmuPdb view: OFF :     Currently no data for PAS domain containing serine/threonine kinase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1323 2q37.3 PASK PAS domain containing serine/threonine kinase
Mouse - 1383 1 D Pask PAS domain containing serine/threonine kinase
Rat - 1385 9 q36 Pask PAS domain containing serine/threonine kinase
Previous and Unofficial Names
PASKIN | STK37
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human PAS kinase bound to ADP
PDB Id:  3DLS
Ligand:  ADP   This ligand is endogenous
Resolution:  2.3Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Structure and interactions of PAS kinase N-terminal PAS domain: Model for intramolecular kinase regulation
PDB Id:  1LL8
Resolution:  0.0Å
Species:  Human
References:  1
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
PP-242 Hs Inhibition - - 3
[3]
Description: Measured as % inhibition at 1μM compound.
Inhibitor Comments
Compound PP-242 inhibits PASK activity by approximately 74% at 1μM [3].
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: PASK/PASK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 3.7 4.5 -1.5
K-252a Hs Inhibitor Inhibition 14.6 14.0 4.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 24.8 63.0 6.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 32.0 40.0 -1.0
isogranulatimide Hs Inhibitor Inhibition 33.6 57.0 26.0
PKR inhibitor Hs Inhibitor Inhibition 40.9 46.0 2.0
SB 218078 Hs Inhibitor Inhibition 43.3 117.0 104.0
JAK3 inhibitor II Hs Inhibitor Inhibition 57.9 73.0 8.0
JNK inhibitor V Hs Inhibitor Inhibition 64.1 90.0 36.0
GF109203X Hs Inhibitor Inhibition 67.0 74.0 18.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Amezcua CA, Harper SM, Rutter J, Gardner KH. (2002) Structure and interactions of PAS kinase N-terminal PAS domain: model for intramolecular kinase regulation. Structure, 10 (10): 1349-61. [PMID:12377121]

2. 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]

3. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat. Chem. Biol., 4 (11): 691-9. [PMID:18849971]

4. 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]

5. Kikani CK, Antonysamy SA, Bonanno JB, Romero R, Zhang FF, Russell M, Gheyi T, Iizuka M, Emtage S, Sauder JM et al.. (2010) Structural bases of PAS domain-regulated kinase (PASK) activation in the absence of activation loop phosphorylation. J. Biol. Chem., 285 (52): 41034-43. [PMID:20943661]

How to cite this page

PASK subfamily: PAS domain containing serine/threonine kinase. Last modified on 24/02/2015. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2139.