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, Altman A (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, Uberall F, Schraven B, Baier G (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, Caothien RH, Pettiford SM, Wellik S, Mandac JB, Kauvar LM (July 1999). "Direct interaction in T-cells between thetaPKC and the tyrosine kinase p59fyn". J. Biol. Chem. 274 (27): 19003–10. 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. 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. PMID 10725744. 
  7. ^ Takeda K, Harada Y, Watanabe R, Inutake Y, Ogawa S, Onuki K, Kagaya S, Tanabe K, Kishimoto H, Abe R (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, Keily SB, Henderson J, Miller A, Pierard F, Settimo L, Twin HC, Bolton CM, Curnock AP, Chiu P, Tanner AJ, Young S (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]