phosphorylase kinase catalytic subunit gamma 1 | Phosphorylase kinase (PHK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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phosphorylase kinase catalytic subunit gamma 1

Target not currently curated in GtoImmuPdb

Target id: 2145

Nomenclature: phosphorylase kinase catalytic subunit gamma 1

Abbreviated Name: PHKG1

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 - 387 7p11.2 PHKG1 phosphorylase kinase catalytic subunit gamma 1
Mouse - 388 5 G1.3 Phkg1 phosphorylase kinase gamma 1
Rat - 388 12 q13 Phkg1 phosphorylase kinase catalytic subunit gamma 1
Previous and Unofficial Names
gamma phosphorylase kinase | HK-gamma-M | PHKIN01 | phosphorylase kinase, gamma 1 (muscle) | phosphorylase kinase gamma subunit 1 | phosphorylase kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
A-443654 Hs Inhibition - - 3
[3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
A-443654 inhibits PHKG1 activity by approximately 76% using 1μM compound [3].
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: PHKG1
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 9.4 pKd
staurosporine Hs Inhibitor Inhibition 9.2 pKd
sunitinib Hs Inhibitor Inhibition 8.3 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
SU-14813 Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Hs Inhibitor Inhibition 6.7 pKd
fedratinib Hs Inhibitor Inhibition 6.5 pKd
bosutinib Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.2 pKd
dovitinib 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
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/PHKg1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 1.2
staurosporine Hs Inhibitor Inhibition 1.4
Gö 6976 Hs Inhibitor Inhibition 1.8
midostaurin Hs Inhibitor Inhibition 2.3
SB 218078 Hs Inhibitor Inhibition 2.7
SU11652 Hs Inhibitor Inhibition 3.2
sunitinib Hs Inhibitor Inhibition 5.1
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 7.7
indirubin derivative E804 Hs Inhibitor Inhibition 8.1
alsterpaullone Hs Inhibitor Inhibition 9.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Glycogen storage disease due to muscle phosphorylase kinase deficiency
Synonyms: Glycogen storage disease IX [Disease Ontology: DOID:0050594]
Disease Ontology: DOID:0050594
Orphanet: ORPHA715

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. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation. Nat. Chem. Biol., 5 (7): 484-93. [PMID:19465931]

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

Phosphorylase kinase (PHK) family: phosphorylase kinase catalytic subunit gamma 1. Last modified on 30/03/2016. Accessed on 21/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2145.