protein kinase C iota | Iota subfamily | IUPHAR Guide to IMMUNOPHARMACOLOGY

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protein kinase C iota

  Target has curated data in GtoImmuPdb

Target id: 1490

Nomenclature: protein kinase C iota

Abbreviated Name: PKCι

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 596 3q26.3 PRKCI protein kinase C iota
Mouse - 595 3 Prkci protein kinase C, iota
Rat - 596 2q24 Prkci protein kinase C
Previous and Unofficial Names
atypical protein kinase C-lambda/iota | Pkcl | protein kinase C
Database Links
BRENDA
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:  Crystal Structure of PKCiota kinase domain
PDB Id:  3A8X
Resolution:  2.0Å
Species:  Human
References:  5
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 Affinity Parameter Reference
staurosporine Hs Inhibition 6.5 pIC50 4
pIC50 6.5 (IC50 3.46x10-7 M) [4]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: PRKCI
Ligand Sp. Type Action Affinity Parameter
staurosporine Hs Inhibitor Inhibition 7.6 pKd
GSK690693 Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Hs Inhibitor Inhibition 5.8 pKd
lestaurtinib Hs Inhibitor Inhibition 5.7 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
linifanib Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
gefitinib 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PKCι/PKCiota
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 4.6 56.5 9.0
Ro-32-0432 Hs Inhibitor Inhibition 36.2
K-252a Hs Inhibitor Inhibition 42.0 107.0 69.0
GF109203X Hs Inhibitor Inhibition 55.9 74.0 47.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 65.3 102.0 67.0
Gö 6983 Hs Inhibitor Inhibition 67.6 89.0 62.0
aloisine Hs Inhibitor Inhibition 72.8 112.0 99.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 74.3 104.0 103.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 78.9 112.0 80.0
PKR inhibitor Hs Inhibitor Inhibition 80.3 85.0 73.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCι is included in GtoImmuPdb based on the involvement of other PKC isozymes in immune processes.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0070555 response to interleukin-1 IEA

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. Qi ZH, Song M, Wallace MJ, Wang D, Newton PM, McMahon T, Chou WH, Zhang C, Shokat KM, Messing RO. (2007) Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. J. Biol. Chem., 282 (45): 33052-63. [PMID:17875639]

5. Takimura T, Kamata K, Fukasawa K, Ohsawa H, Komatani H, Yoshizumi T, Takahashi I, Kotani H, Iwasawa Y. (2010) Structures of the PKC-iota kinase domain in its ATP-bound and apo forms reveal defined structures of residues 533-551 in the C-terminal tail and their roles in ATP binding. Acta Crystallogr. D Biol. Crystallogr., 66 (Pt 5): 577-83. [PMID:20445233]

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

Iota subfamily: protein kinase C iota. Last modified on 22/03/2017. Accessed on 20/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1490.