phosphorylase kinase catalytic subunit gamma 2 | Phosphorylase kinase (PHK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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phosphorylase kinase catalytic subunit gamma 2

Target not currently curated in GtoImmuPdb

Target id: 2147

Nomenclature: phosphorylase kinase catalytic subunit gamma 2

Abbreviated Name: PHKG2

Family: Phosphorylase kinase (PHK) 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 - 406 16p11.2 PHKG2 phosphorylase kinase catalytic subunit gamma 2
Mouse - 406 7 F4 Phkg2 phosphorylase kinase
Rat - 406 1 q36 Phkg2 phosphorylase kinase catalytic subunit gamma 2
Previous and Unofficial Names
PHK-gamma-LT | PHK-gamma-T | PSK-C3 | phosphorylase kinase, gamma 2 (testis) | phosphorylase kinase gamma subunit 2 | phosphorylase kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human phosphorylase kinase, gamma 2
PDB Id:  2Y7J
Resolution:  2.5Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.19

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 Value Parameter Reference
staurosporine Hs Inhibition 10.0 pIC50 4
pIC50 10.0 (IC50 1x10-10 M) [4]
compound 2c [PMID: 24900538] Hs Inhibition 8.2 pIC50 5
pIC50 8.2 (IC50 6.1x10-9 M) [5]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: PHKG2
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.9 pKd
lestaurtinib Hs Inhibitor Inhibition 8.8 pKd
sunitinib Hs Inhibitor Inhibition 8.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.9 pKd
SU-14813 Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Hs Inhibitor Inhibition 6.8 pKd
BMS-387032 Hs Inhibitor Inhibition 6.3 pKd
afatinib Hs Inhibitor Inhibition 6.3 pKd
PP-242 Hs Inhibitor Inhibition 6.1 pKd
tamatinib Hs Inhibitor Inhibition 6.0 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PhKγ2/PHKg2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 3.4 3.5 1.0
K-252a Hs Inhibitor Inhibition 6.5 0.0 1.0
Gö 6976 Hs Inhibitor Inhibition 8.4 1.0 2.0
SU11652 Hs Inhibitor Inhibition 16.6 8.0 2.0
sunitinib Hs Inhibitor Inhibition 20.6
dorsomorphin Hs Inhibitor Inhibition 31.2 34.0 4.0
indirubin derivative E804 Hs Inhibitor Inhibition 34.9 21.0 5.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 47.0 22.0 3.0
Syk inhibitor Hs Inhibitor Inhibition 52.0 24.0 9.0
JAK inhibitor I Hs Inhibitor Inhibition 57.3 41.0 24.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Glycogen storage disease IXc
Synonyms: Glycogen storage disease due to liver phosphorylase kinase deficiency [Orphanet: ORPHA264580]
Glycogen storage disease IX [Disease Ontology: DOID:0050594]
Disease Ontology: DOID:0050594
OMIM: 613027
Orphanet: ORPHA264580

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. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J. Med. Chem., 52 (10): 3191-204. [PMID:19397322]

5. Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD et al.. (2012) Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett, 3 (9): 705-9. [PMID:24900538]

6. 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

Phosphorylase kinase (PHK) family: phosphorylase kinase catalytic subunit gamma 2. Last modified on 30/03/2016. Accessed on 08/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2147.