protein kinase AMP-activated catalytic subunit alpha 2 | AMPK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase AMP-activated catalytic subunit alpha 2

Target not currently curated in GtoImmuPdb

Target id: 1542

Nomenclature: protein kinase AMP-activated catalytic subunit alpha 2

Abbreviated Name: AMPKA2

Family: AMPK subfamily

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 - 552 1p31 PRKAA2 protein kinase AMP-activated catalytic subunit alpha 2
Mouse - 552 4 Prkaa2 protein kinase
Rat - 552 5q34 Prkaa2 protein kinase AMP-activated catalytic subunit alpha 2
Previous and Unofficial Names
AMPK alpha-2 chain | ACACA kinase | acetyl-CoA carboxylase kinase | AMP kinase α2 subunit | HMGCR kinase | hydroxymethylglutaryl-CoA reductase kinase | AMPKa2 | AMP-activated protein kinase, alpha 2 catalytic subunit | protein kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Protein Kinase Domain of the Human 5'-AMP-activated protein kinase catalytic subunit alpha-2 (AMPK alpha-2 chain)
PDB Id:  2H6D
Resolution:  1.85Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.1
DiscoveRx KINOMEscan® screen
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: AMPK-alpha2
Ligand Sp. Type Action Value Parameter
JNJ-28312141 Hs Inhibitor Inhibition 8.4 pKd
staurosporine Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 7.3 pKd
sunitinib Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Hs Inhibitor Inhibition 6.5 pKd
tozasertib Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
midostaurin Hs Inhibitor Inhibition 6.3 pKd
tamatinib Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
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...

Key to terms and symbols Click column headers to sort
Target used in screen: AMPKα2/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition -5.0 1.0
Tpl2 kinase inhibitor Hs Inhibitor Inhibition -5.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition -3.0 0.0
staurosporine Hs Inhibitor Inhibition -2.5 1.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 1.0 3.0
midostaurin Hs Inhibitor Inhibition 1.0 4.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 1.0 10.0
PKR inhibitor Hs Inhibitor Inhibition 3.0 3.0
indirubin derivative E804 Hs Inhibitor Inhibition 3.0 4.0
SU11652 Hs Inhibitor Inhibition 4.0 4.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. 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]

3. Littler DR, Walker JR, Davis T, Wybenga-Groot LE, Finerty PJ, Newman E, Mackenzie F, Dhe-Paganon S. (2010) A conserved mechanism of autoinhibition for the AMPK kinase domain: ATP-binding site and catalytic loop refolding as a means of regulation. Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun., 66 (Pt 2): 143-51. [PMID:20124709]

4. 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

AMPK subfamily: protein kinase AMP-activated catalytic subunit alpha 2. Last modified on 30/03/2016. Accessed on 25/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1542.