protein kinase C zeta | Iota subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase C zeta

Target id: 1491

Nomenclature: protein kinase C zeta

Abbreviated Name: PKCζ

Family: Iota subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     protein kinase C zeta has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 409 1p36.33-p36.2 PRKCZ protein kinase C zeta
Mouse - 592 4 E2 Prkcz protein kinase C, zeta
Rat - 592 5 q36 Prkcz protein kinase C, zeta
Previous and Unofficial Names
PKC2 | aPKCzeta | protein kinase C
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.13

Download all structure-activity data for this target as a CSV file

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
arachidonic acid Hs Activation - - 5
[5]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 3 [PMID: 19097791] Hs Inhibition 8.6 pIC50 6
pIC50 8.6 (IC50 2.26x10-9 M) [6]
Gö 6983 Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 6x10-8 M) [4]
balanol Hs Inhibition 5.2 pIC50 2
pIC50 5.2 (IC50 5.9x10-6 M) [2]
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: PKCζ/PKCzeta
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 22.0 18.5 5.0
Ro-32-0432 Hs Inhibitor Inhibition 31.0
GF109203X Hs Inhibitor Inhibition 57.2 72.0 16.0
vatalanib Hs Inhibitor Inhibition 69.5
K-252a Hs Inhibitor Inhibition 70.1 52.0 8.0
tozasertib Hs Inhibitor Inhibition 76.4
Gö 6983 Hs Inhibitor Inhibition 78.2 82.0 27.0
lapatinib Hs Inhibitor Inhibition 79.7
H-89 Hs Inhibitor Inhibition 79.8 99.0 78.0
dovitinib 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
GO Annotations:  Associated to 3 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS
GO:2000553 positive regulation of T-helper 2 cell cytokine production ISS
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS
GO:2000553 positive regulation of T-helper 2 cell cytokine production ISS
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:2000553 positive regulation of T-helper 2 cell cytokine production ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS
GO:2000553 positive regulation of T-helper 2 cell cytokine production ISS
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 5 GO processes
GO:0032753 positive regulation of interleukin-4 production ISS
GO:2000553 positive regulation of T-helper 2 cell cytokine production ISS
GO:2000664 positive regulation of interleukin-5 secretion ISS
GO:2000667 positive regulation of interleukin-13 secretion ISS
GO:2001181 positive regulation of interleukin-10 secretion ISS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0045630 positive regulation of T-helper 2 cell differentiation ISS

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 22/03/2017. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1491.