protein kinase C gamma | Alpha subfamily | IUPHAR Guide to IMMUNOPHARMACOLOGY

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protein kinase C gamma

  Target has curated data in GtoImmuPdb

Target id: 1484

Nomenclature: protein kinase C gamma

Abbreviated Name: PKCγ

Family: Alpha 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 - 697 19q13.4 PRKCG protein kinase C gamma
Mouse - 697 7 Prkcg protein kinase C
Rat - 697 1q12 Prkcg protein kinase C
Previous and Unofficial Names
PKCC | SCA14 | PKC-gamma | PKCI | Prkcc | protein kinase C, gamma | protein kinase C
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of the phorbol esters/diacylglycerol binding domain of protein kinase C gamma
PDB Id:  2E73
Resolution:  0.0Å
Species:  Human
References: 
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 Parameter Reference
ingenol mebutate Hs Activation 9.8 pKi 8
pKi 9.8 (Ki 1.62x10-10 M) [8]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
Gö 6983 Hs Inhibition 8.2 pIC50 6
pIC50 8.2 (IC50 6x10-9 M) [6]
balanol Hs Inhibition 8.0 pIC50 3
pIC50 8.0 (IC50 1x10-8 M) [3]
GF109203X Bt Inhibition 7.7 pIC50 10
pIC50 7.7 (IC50 2x10-8 M) [10]
7-hydroxystaurosporine Hs Inhibition 7.5 pIC50 9
pIC50 7.5 (IC50 3x10-8 M) [9]
Ro-32-0432 Bt Inhibition 7.4 – 7.4 pIC50 2,11
pIC50 7.4 – 7.4 (IC50 3.7x10-8 – 3.65x10-8 M) [2,11]
ruboxistaurin Hs Inhibition 6.5 pIC50 7
pIC50 6.5 (IC50 3x10-7 M) [7]
enzastaurin Hs Inhibition 5.7 pIC50 4
pIC50 5.7 (IC50 2x10-6 M) [4]
View species-specific inhibitor tables
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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: PKCγ/PKCg
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition -3.2 1.5 1.0
Ro-32-0432 Hs Inhibitor Inhibition 6.9
GF109203X Hs Inhibitor Inhibition 17.6 1.0 1.0
SB 218078 Hs Inhibitor Inhibition 32.8 92.0 96.0
midostaurin Hs Inhibitor Inhibition 35.6 15.0 6.0
K-252a Hs Inhibitor Inhibition 40.2 19.0 2.0
PKCbeta inhibitor Hs Inhibitor Inhibition 51.6 8.0 2.0
Gö 6983 Hs Inhibitor Inhibition 54.0 3.0 0.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 59.3 113.0 95.0
Gö 6976 Hs Inhibitor Inhibition 72.1 9.0 16.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCγ is included in GtoImmuPdb based on the involvement of other PKC isozymes in immune processes.
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0031397 negative regulation of protein ubiquitination IDA
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050764 regulation of phagocytosis IEA
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050764 regulation of phagocytosis IEA
Clinically-Relevant Mutations and Pathophysiology
Disease:  Spinocerebellar ataxia 14; SCA14
Synonyms: Spinocerebellar ataxia [Disease Ontology: DOID:1441]
Disease Ontology: DOID:1441
OMIM: 605361
Orphanet: ORPHA98763

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. Birchall AM, Bishop J, Bradshaw D, Cline A, Coffey J, Elliott LH, Gibson VM, Greenham A, Hallam TJ, Harris W et al.. (1994) Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J. Pharmacol. Exp. Ther., 268 (2): 922-9. [PMID:8114006]

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. Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M. (2003) Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg. Med. Chem. Lett., 13 (11): 1857-9. [PMID:12749884]

5. 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]

6. 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]

7. Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH, Neel DA, Rito CJ, Singh U, Stramm LE, Melikian-Badalian A et al.. (1996) (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J. Med. Chem., 39 (14): 2664-71. [PMID:8709095]

8. Kedei N, Lundberg DJ, Toth A, Welburn P, Garfield SH, Blumberg PM. (2004) Characterization of the interaction of ingenol 3-angelate with protein kinase C. Cancer Res., 64 (9): 3243-55. [PMID:15126366]

9. Seynaeve CM, Kazanietz MG, Blumberg PM, Sausville EA, Worland PJ. (1994) Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue. Mol. Pharmacol., 45 (6): 1207-14. [PMID:8022414]

10. Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F et al.. (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J. Biol. Chem., 266 (24): 15771-81. [PMID:1874734]

11. Wilkinson SE, Parker PJ, Nixon JS. (1993) Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem. J., 294 ( Pt 2): 335-7. [PMID:8373348]

How to cite this page

Alpha subfamily: protein kinase C gamma. Last modified on 22/03/2017. Accessed on 19/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1484.