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protein kinase C zeta

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Target id: 1491

Nomenclature: protein kinase C zeta

Abbreviated Name: PKCζ

Family: Iota subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 592 1p36.33 PRKCZ protein kinase C zeta
Mouse - 592 4 86.17 cM Prkcz protein kinase C, zeta
Rat - 592 5q36 Prkcz protein kinase C, zeta
Previous and Unofficial Names Click here for help
PKC2 | aPKCzeta | protein kinase C
Database Links Click here for help
Alphafold Q05513 (Hs), Q02956 (Mm), P09217 (Rn)
BRENDA 2.7.11.13
ChEMBL Target CHEMBL3438 (Hs)
Ensembl Gene ENSG00000067606 (Hs), ENSMUSG00000029053 (Mm), ENSRNOG00000015480 (Rn)
Entrez Gene 5590 (Hs), 18762 (Mm), 25522 (Rn)
Human Protein Atlas ENSG00000067606 (Hs)
KEGG Enzyme 2.7.11.13
KEGG Gene hsa:5590 (Hs), mmu:18762 (Mm), rno:25522 (Rn)
OMIM 176982 (Hs)
Pharos Q05513 (Hs)
RefSeq Nucleotide NM_001033581 (Hs), NM_008860 (Mm), NM_022507 (Rn)
RefSeq Protein NP_001028753 (Hs), NP_032886 (Mm), NP_001034168 (Mm), NP_071952 (Rn)
UniProtKB Q05513 (Hs), Q02956 (Mm), P09217 (Rn)
Wikipedia PRKCZ (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.13

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

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
arachidonic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Activation - - 5
⤷ [5]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 3 [PMID: 19097791] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pIC50 6
⤷ pIC50 8.6 (IC50 2.26x10-9 M) [6]
Gö 6983 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pIC50 4
⤷ pIC50 7.2 (IC50 6x10-8 M) [4]
balanol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.2 pIC50 2
⤷ pIC50 5.2 (IC50 5.9x10-6 M) [2]
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: PKCζ/PKCzeta
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 22.0 18.5 5.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 31.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 57.2 72.0 16.0
vatalanib Small molecule or natural product Hs Inhibitor Inhibition 69.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 70.1 52.0 8.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 76.4
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 78.2 82.0 27.0
lapatinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 79.7
H-89 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 79.8 99.0 78.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 81.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCζ is included in GtoImmuPdb based on its GO process associations.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling

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. Defauw JM, Murphy MM, Jagdmann Jr GE, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS et al.. (1996) Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. J Med Chem, 39 (26): 5215-27. [PMID:8978850]

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. Gschwendt M, Dieterich S, Rennecke J, Kittstein W, Mueller HJ, Johannes FJ. (1996) Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett, 392 (2): 77-80. [PMID:8772178]

5. Müller G, Ayoub M, Storz P, Rennecke J, Fabbro D, Pfizenmaier K. (1995) PKC zeta is a molecular switch in signal transduction of TNF-alpha, bifunctionally regulated by ceramide and arachidonic acid. EMBO J, 14 (9): 1961-9. [PMID:7744003]

6. Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA et al.. (2009) 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. Bioorg Med Chem Lett, 19 (3): 908-11. [PMID:19097791]

How to cite this page

Iota subfamily: protein kinase C zeta. Last modified on 09/06/2021. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1491.