PRKCQ

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Protein kinase C, theta
Protein PRKCQ PDB 1xjd.png
PDB rendering based on 1xjd.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols PRKCQ ; PRKCT; nPKC-theta
External IDs OMIM600448 MGI97601 HomoloGene21263 ChEMBL: 3920 GeneCards: PRKCQ Gene
EC number 2.7.11.13
RNA expression pattern
PBB GE PRKCQ 210039 s at tn.png
PBB GE PRKCQ 210038 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 5588 18761
Ensembl ENSG00000065675 ENSMUSG00000026778
UniProt Q04759 Q02111
RefSeq (mRNA) NM_001242413 NM_008859
RefSeq (protein) NP_001229342 NP_032885
Location (UCSC) Chr 10:
6.47 – 6.62 Mb
Chr 2:
11.17 – 11.3 Mb
PubMed search [1] [2]

Protein kinase C theta (PKC-θ) is an enzyme that in humans is encoded by the PRKCQ gene.[1]

Function[edit]

Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by the second messenger diacylglycerol. PKC family members phosphorylate a wide variety of protein targets and are known to be involved in diverse cellular signaling pathways. PKC family members also serve as major receptors for phorbol esters, a class of tumor promoters. Each member of the PKC family has a specific expression profile and is believed to play a distinct role. The protein encoded by this gene is one of the PKC family members. It is a calcium-independent and phospholipid-dependent protein kinase. This kinase is important for T-cell activation. It is required for the activation of the transcription factors NF-kappaB and AP-1, and may link the T cell receptor (TCR) signaling complex to the activation of the transcription factors.[2]

Interactions[edit]

PRKCQ has been shown to interact with:

PRKCQ has been shown to phosphorylate CARD11 as part of the NF-κB signaling pathway.[7]

Inhibitors[edit]

  • (R)-2-((S)-4-(3-Chloro-5-fluoro-6-(1H-pyrazolo[3,4-b]pyridin- 3-yl)pyridin-2-yl)piperazin-2-yl)-3-methylbutan-2-ol[8]

See also[edit]

References[edit]

  1. ^ Baier G, Telford D, Giampa L, Coggeshall KM, Baier-Bitterlich G, Isakov N et al. (April 1993). "Molecular cloning and characterization of PKC theta, a novel member of the protein kinase C (PKC) gene family expressed predominantly in hematopoietic cells". J Biol Chem 268 (7): 4997–5004. PMID 8444877. 
  2. ^ "Entrez Gene: PRKCQ protein kinase C, theta". 
  3. ^ Bauer B, Krumböck N, Fresser F, Hochholdinger F, Spitaler M, Simm A et al. (August 2001). "Complex formation and cooperation of protein kinase C theta and Akt1/protein kinase B alpha in the NF-kappa B transactivation cascade in Jurkat T cells". J. Biol. Chem. 276 (34): 31627–34. doi:10.1074/jbc.M103098200. PMID 11410591. 
  4. ^ Ron D, Napolitano EW, Voronova A, Vasquez NJ, Roberts DN, Calio BL et al. (July 1999). "Direct interaction in T-cells between thetaPKC and the tyrosine kinase p59fyn". J. Biol. Chem. 274 (27): 19003–10. doi:10.1074/jbc.274.27.19003. PMID 10383400. 
  5. ^ Witte S, Villalba M, Bi K, Liu Y, Isakov N, Altman A (January 2000). "Inhibition of the c-Jun N-terminal kinase/AP-1 and NF-kappaB pathways by PICOT, a novel protein kinase C-interacting protein with a thioredoxin homology domain". J. Biol. Chem. 275 (3): 1902–9. doi:10.1074/jbc.275.3.1902. PMID 10636891. 
  6. ^ Hehner SP, Li-Weber M, Giaisi M, Dröge W, Krammer PH, Schmitz ML (April 2000). "Vav synergizes with protein kinase C theta to mediate IL-4 gene expression in response to CD28 costimulation in T cells". J. Immunol. 164 (7): 3829–36. doi:10.4049/jimmunol.164.7.3829. PMID 10725744. 
  7. ^ Takeda K, Harada Y, Watanabe R, Inutake Y, Ogawa S, Onuki K et al. (December 2008). "CD28 stimulation triggers NF-kappaB activation through the CARMA1-PKCtheta-Grb2/Gads axis.". Int. Immunol. 20 (12): 1507–15. doi:10.1093/intimm/dxn108. PMID 18829987. 
  8. ^ Jimenez JM, Boyall D, Brenchley G, Collier PN, Davis CJ, Fraysse D et al. (2013). "Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases". J. Med. Chem. 56 (5): 1799–810. doi:10.1021/jm301465a. PMID 23398373. 

Further reading[edit]