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protein kinase C iota

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1490

Nomenclature: protein kinase C iota

Abbreviated Name: PKCι

Family: Iota subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 596 3q26.2 PRKCI protein kinase C iota
Mouse - 595 3 14.65 cM Prkci protein kinase C, iota
Rat - 596 2q24 Prkci protein kinase C, iota
Previous and Unofficial Names Click here for help
atypical protein kinase C-lambda/iota | Pkcl | protein kinase C
Database Links Click here for help
Alphafold P41743 (Hs), Q62074 (Mm), F1M7Y5 (Rn)
BRENDA 2.7.11.13
ChEMBL Target CHEMBL2598 (Hs)
Ensembl Gene ENSG00000163558 (Hs), ENSMUSG00000037643 (Mm), ENSRNOG00000009652 (Rn)
Entrez Gene 5584 (Hs), 18759 (Mm), 84006 (Rn)
Human Protein Atlas ENSG00000163558 (Hs)
KEGG Enzyme 2.7.11.13
KEGG Gene hsa:5584 (Hs), mmu:18759 (Mm), rno:84006 (Rn)
OMIM 600539 (Hs)
Pharos P41743 (Hs)
RefSeq Nucleotide NM_002740 (Hs), NM_008857 (Mm), NM_032059 (Rn)
RefSeq Protein NP_002731 (Hs), NP_032883 (Mm), NP_114448 (Rn)
UniProtKB P41743 (Hs), Q62074 (Mm), F1M7Y5 (Rn)
Wikipedia PRKCI (Hs)
Selected 3D Structures Click here for help
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 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

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 6.5 pIC50 4
⤷ pIC50 6.5 (IC50 3.46x10-7 M) [4]
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: PRKCI
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 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: PKCι/PKCiota
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 4.6 56.5 9.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 36.2
K-252a Small molecule or natural product Hs Inhibitor Inhibition 42.0 107.0 69.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 55.9 74.0 47.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 65.3 102.0 67.0
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 67.6 89.0 62.0
aloisine Small molecule or natural product Hs Inhibitor Inhibition 72.8 112.0 99.0
GSK-3 inhibitor X Small molecule or natural product Hs Inhibitor Inhibition 74.3 104.0 103.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.9 112.0 80.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure 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

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 09/06/2021. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1490.