Delta subfamily | Enzymes | IUPHAR/BPS Guide to MALARIA PHARMACOLOGY

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Delta subfamily C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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PKCδ and PKCθ are PKC isoforms that are activated by diacylglycerol and may be inhibited by calphostin C, Gö 6983 and chelerythrine.

Enzymes

PKCα (protein kinase C alpha) C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1482

Nomenclature

protein kinase C alpha

Common abbreviation

PKCα

Previous and unofficial names

PKC-alpha | protein kinase C

Genes

PRKCA (Hs), Prkca (Mm), Prkca (Rn)

Ensembl ID

ENSG00000154229 (Hs), ENSMUSG00000050965 (Mm), ENSRNOG00000003491 (Rn)

UniProtKB AC

P17252 (Hs), P20444 (Mm), P05696 (Rn)

EC number

2.7.11.13

Inhibitors

sotrastaurin pIC₅₀ 8.7 [10]

Gö 6983 pIC₅₀ 8.1 [2]

7-hydroxystaurosporine pIC₅₀ 7.5 [8]

Comment

Protein interacting with PRKCA 1 (PICK1: Q9NRD5) appears to act as an adaptor/scaffold protein that affects the localisation and function of PRKCA and other receptor/channel proteins through protein-protein interactions that are mediated by the PICK1 PDZ domain [5,7,9,11]. PICK1 is proposed as a target for pain modulation [1], with peptide inhibitors of the PICK1-PRKCA interaction reported to provide relief from chronic pain in mouse models [3,6].

PKCδ (protein kinase C delta) C Show summary »« Hide summary More detailed page go icon to follow link

PKCθ (protein kinase C theta) C Show summary »« Hide summary More detailed page go icon to follow link

References

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1. Christensen NR, De Luca M, Lever MB, Richner M, Hansen AB, Noes-Holt G, Jensen KL, Rathje M, Jensen DB, Erlendsson S et al.. (2020) A high-affinity, bivalent PDZ domain inhibitor complexes PICK1 to alleviate neuropathic pain. EMBO Mol Med, 12 (6): e11248. [PMID:32352640]

2. 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]

3. Jensen KL, Christensen NR, Goddard CM, Jager SE, Noes-Holt G, Kanneworff IB, Jakobsen A, Jiménez-Fernández L, Peck EG, Sivertsen L et al.. (2024) Peripherally restricted PICK1 inhibitor mPD5 ameliorates pain behaviors in murine inflammatory and neuropathic pain models. JCI Insight, 9 (20). [PMID:39287978]

4. 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]

5. Madsen KL, Beuming T, Niv MY, Chang CW, Dev KK, Weinstein H, Gether U. (2005) Molecular determinants for the complex binding specificity of the PDZ domain in PICK1. J Biol Chem, 280 (21): 20539-48. [PMID:15774468]

6. Noes-Holt G, Jensen KL, Comaposada-Baró R, Jager SE, Richner M, Goddard CM, Kowenicki MBK, Sivertsen L, Jiménez-Fernández L, Andersen RC et al.. (2026) Recombinant dimeric PICK1 peptide inhibitors for long-term relief of chronic pain by AAV therapeutics. Cell Rep Med,: 102800 [Epub ahead of print]. [PMID:42134332]

7. Perez JL, Khatri L, Chang C, Srivastava S, Osten P, Ziff EB. (2001) PICK1 targets activated protein kinase Calpha to AMPA receptor clusters in spines of hippocampal neurons and reduces surface levels of the AMPA-type glutamate receptor subunit 2. J Neurosci, 21 (15): 5417-28. [PMID:11466413]

8. 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]

9. Shao X, Zhu L, Wang Y, Lu Y, Wang W, Zhu J, Shen Y, Xia J, Luo J. (2010) Threonine 82 at the PDZ domain of PICK1 is critical for AMPA receptor interaction and localization. Neurochem Int, 56 (8): 962-70. [PMID:20403402]

10. Wagner J, von Matt P, Sedrani R, Albert R, Cooke N, Ehrhardt C, Geiser M, Rummel G, Stark W, Strauss A et al.. (2009) Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. J Med Chem, 52 (20): 6193-6. [PMID:19827831]

11. Yu N, Wang X, Bao H, Liu Z. (2019) Identification and functional study of three nAChR regulators, ubiquilin-1, PICK1, and CRELD2, in Locusta migratoria manilensis dorsal unpaired median neurons. J Neurochem, 149 (3): 331-345. [PMID:30485436]

NC-IUPHAR subcommittee and family contributors

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Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Gibb AJ, Kelly E, Mathie AA, Peach CJ, Veale EL, Armstrong JF, Faccenda E, Harding SD, Southan C, Davies JA et al. (2025) The Concise Guide to PHARMACOLOGY 2025/26: Enzymes. Br J Pharmacol. 182: S307-S403.