protein kinase C eta | Eta subfamily | IUPHAR Guide to IMMUNOPHARMACOLOGY

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protein kinase C eta

  Target has curated data in GtoImmuPdb

Target id: 1487

Nomenclature: protein kinase C eta

Abbreviated Name: PKCη

Family: Eta subfamily

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 - 683 14q23.1 PRKCH protein kinase C eta
Mouse - 683 12 C3-D1 Prkch protein kinase C, eta
Rat - 683 6q24 Prkch protein kinase C, eta
Previous and Unofficial Names
PKCL | PKC-L | PRKCL | Pkch | protein kinase C, eta | protein kinase C
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human protein kinase C, eta
PDB Id:  2FK9
Resolution:  1.75Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  PKC eta kinase in complex with a naphthyridine
PDB Id:  3TXO
Resolution:  2.05Å
Species:  Human
References:  7
Enzyme Reaction
EC Number: 2.7.11.13

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
balanol Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3x10-9 M) [3]
sotrastaurin Hs Inhibition 8.2 pIC50 8
pIC50 8.2 (IC50 6.1x10-9 M) [8]
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: 2,9

Key to terms and symbols Click column headers to sort
Target used in screen: PRKCH
Ligand Sp. Type Action Value Parameter
GSK690693 Hs Inhibitor Inhibition 8.6 pKd
staurosporine Hs Inhibitor Inhibition 8.3 pKd
A-674563 Hs Inhibitor Inhibition 8.0 pKd
enzastaurin Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 6.8 pKd
midostaurin Hs Inhibitor Inhibition 6.5 pKd
alvocidib Hs Inhibitor Inhibition 6.5 pKd
PP-242 Hs Inhibitor Inhibition 6.1 pKd
ruboxistaurin Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition <5.5 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: PKCη/PKCeta
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.4 2.5 0.0
Gö 6983 Hs Inhibitor Inhibition 6.8 10.0 2.0
GF109203X Hs Inhibitor Inhibition 7.7 9.0 1.0
Ro-32-0432 Hs Inhibitor Inhibition 7.8
midostaurin Hs Inhibitor Inhibition 20.4 84.0 29.0
K-252a Hs Inhibitor Inhibition 20.5 36.0 7.0
PKCbeta inhibitor Hs Inhibitor Inhibition 29.7 15.0 2.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 34.4 27.0 4.0
Gö 6976 Hs Inhibitor Inhibition 35.3 72.0 60.0
PKR inhibitor Hs Inhibitor Inhibition 41.2 23.0 5.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCη is included in GtoImmuPdb based on the involvement of other PKC isozymes in immune processes.
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050861 positive regulation of B cell receptor signaling pathway IMP
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0050861 positive regulation of B cell receptor signaling pathway IMP
Clinically-Relevant Mutations and Pathophysiology
Disease:  Stroke, ischemic
Synonyms: Cerebral infarction
Cerebrovascular accident [Disease Ontology: DOID:3455]
Disease Ontology: DOID:3455
OMIM: 601367
Comments: 
References:  5
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human V374I 1425G>A 5

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. 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]

4. 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]

5. Kubo M, Hata J, Ninomiya T, Matsuda K, Yonemoto K, Nakano T, Matsushita T, Yamazaki K, Ohnishi Y, Saito S et al.. (2007) A nonsynonymous SNP in PRKCH (protein kinase C eta) increases the risk of cerebral infarction. Nat. Genet., 39 (2): 212-7. [PMID:17206144]

6. Littler DR, Walker JR, She YM, Finerty PJ, Newman EM, Dhe-Paganon S. (2006) Structure of human protein kinase C eta (PKCeta) C2 domain and identification of phosphorylation sites. Biochem. Biophys. Res. Commun., 349 (4): 1182-9. [PMID:16973127]

7. van Eis MJ, Evenou JP, Floersheim P, Gaul C, Cowan-Jacob SW, Monovich L, Rummel G, Schuler W, Stark W, Strauss A et al.. (2011) 2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes. Bioorg. Med. Chem. Lett., 21 (24): 7367-72. [PMID:22078216]

8. Wagner J, von Matt P, Sedrani R, Albert R, Cooke N, Ehrhardt C, Geiser M, Rummel G, Stark W, Strauss A et al.. (2009) Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. J. Med. Chem., 52 (20): 6193-6. [PMID:19827831]

9. 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

Eta subfamily: protein kinase C eta. Last modified on 22/03/2017. Accessed on 22/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1487.