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phosphorylase kinase catalytic subunit gamma 2

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Target id: 2147

Nomenclature: phosphorylase kinase catalytic subunit gamma 2

Abbreviated Name: PHKG2

Family: Phosphorylase kinase (PHK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 406 16p11.2 PHKG2 phosphorylase kinase catalytic subunit gamma 2
Mouse - 406 7 F3 Phkg2 phosphorylase kinase, gamma 2 (testis)
Rat - 406 1q37 Phkg2 phosphorylase kinase catalytic subunit gamma 2
Previous and Unofficial Names Click here for help
PHK-gamma-LT | PHK-gamma-T | PSK-C3 | phosphorylase kinase, gamma 2 (testis) | phosphorylase kinase gamma subunit 2 | phosphorylase kinase
Database Links Click here for help
Alphafold P15735 (Hs), Q9DB30 (Mm), P31325 (Rn)
BRENDA 2.7.11.19
ChEMBL Target CHEMBL2349 (Hs)
Ensembl Gene ENSG00000156873 (Hs), ENSMUSG00000030815 (Mm), ENSRNOG00000018725 (Rn)
Entrez Gene 5261 (Hs), 68961 (Mm), 140671 (Rn)
Human Protein Atlas ENSG00000156873 (Hs)
KEGG Enzyme 2.7.11.19
KEGG Gene hsa:5261 (Hs), mmu:68961 (Mm), rno:140671 (Rn)
OMIM 172471 (Hs)
Orphanet ORPHA159810 (Hs)
Pharos P15735 (Hs)
RefSeq Nucleotide NM_000294 (Hs), NM_026888 (Mm), NM_080584 (Rn)
RefSeq Protein NP_000285 (Hs), NP_081164 (Mm), NP_542151 (Rn)
UniProtKB P15735 (Hs), Q9DB30 (Mm), P31325 (Rn)
Wikipedia PHKG2 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.19

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
staurosporine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 10.0 pIC50 4
⤷ pIC50 10.0 (IC50 1x10-10 M) [4]
compound 2c [PMID: 24900538] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 5
⤷ pIC50 8.2 (IC50 6.1x10-9 M) [5]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.9 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
afatinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.4 3.5 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 6.5 0.0 1.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 1.0 2.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.6 8.0 2.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 20.6
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 31.2 34.0 4.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 34.9 21.0 5.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 47.0 22.0 3.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 52.0 24.0 9.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2147.