Inhibition of protein kinase C μ by various inhibitors. Inhibition from protein kinase c isoenzymes
Open accessAbstract
Various inhibitors were tested for their potential to suppress the kinase activity of protein kinase C μ (PKCμ) in vitro and in vivo. Among the staurosporine‐derived, rather selective PKC inhibitors the indolocarbazole Gö 6976 previously shown to inhibit preferentially cPKC isotypes proved to be a potent inhibitor of PKCμ with an IC 5 of 20 nM, whereas the bisindolymaleimide Gö 6983 was extremely ineffective in suppressing PKCμ kinase activity with a thousand‐fold higher ICm of 20 μM. Other strong inhibitors of PKCμ were the rather unspecific inhibitors staurosporine and K252a. Contrary to the poor inhibition of PKCμ by Gö 6983, this compound was found to suppress in vitro kinase activity of PKC isoenzymes from all three subgroups very effectively with IC 50 values from 7 to 60 nM. Thus, Gö 6983 was able to differentiate between PKCμ and other PKC isoenzymes being useful for selective determination of PKCμ kinase activity in the presence of other PKC isoenzymes.
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The observed change in mEPSC amplitude likely reflects postsynaptic modulation of AMPA receptor-mediated currents, not an effect of OT on spontaneous circuit activity per se.
“The change in mEPSC amplitude observed likely reflects a postsynaptic modulation of AMPA receptor mediated currents63 but not an effect of OT on the spontaneous circuit activity per se.”
From Insular cortex mediates approach and avoidance responses to social affective stimuli (2018) · cites this paper as [63]
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- Authors
- Gschwendt, M., Dieterich, S., Rennecke, J., Kittstein, W., Mueller, H.-J., & Johannes, F.-J.
- Affiliations
- German Cancer Research Center (DE)
- University of Stuttgart (DE)
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1996-08-26
- Volume
- 392
- Issue
- 2
- Pages
- 77-80
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2041797033
- Cited by
- 644
- References
- 21
- Citations by year
- 2026: 16 · 2025: 10 · 2024: 11 · 2023: 11 · 2022: 9 · 2021: 13 · 2020: 10 · 2019: 13 · 2018: 14 · 2017: 16 · 2016: 18 · 2015: 14 · 2014: 21 · 2013: 23 · 2012: 20
- FWCI
- 4.29
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- FEBS Letters (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Deutsche Forschungsgemeinschaft
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Signaling Pathways in Disease
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
- Keywords
- PKC inhibitors, Gö6976, staurosporine, K252a, PKC isoforms, kinase inhibition, bisindolylmaleimide, indolocarbazole
- MeSH terms
- Amino Acid Sequence, Animals, Cell Line, Enzyme Activation, Enzyme Inhibitors, Isoenzymes, Molecular Sequence Data, Protein Kinase C, Recombinant Proteins, 3T3 Cells, Mice
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