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The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase‐1β (Rsk‐2) and p70 S6 kinase
Abstract
The protein kinase C (PKC) inhibitors Ro 318220 and GF 109203X have been used in over 350 published studies to investigate the physiological roles of PKC. Here we demonstrate that these inhibitors are not selective for PKC isoforms as was previously assumed. Ro 318220 inhibited MAPKAP kinase‐1β (also known as Rsk‐2) in vitro (IC 50 3 nM) more potently than it inhibited mixed PKC isoforms (IC 50 5 nM), and it also inhibited p70 S6 kinase (IC 50 15 nM). GF 109203X also potently inhibited MAPKAP kinase‐1β (IC 50 50 nM) and p70 S6 kinase (IC 50 100 nM) with similar potency to PKC isoforms (IC 50 30 nM). The inhibition of MAPKAP kinase‐1β, p70 S6 kinase, and probably other protein kinases, may explain many of the effects previously attributed to PKC.
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Alessi, D. R., Gomez, N., Moorhead, G., Lewis, T., Keyse, S. M., & Cohen, P. (1995) · Current Biology · doi:10.1016/s0960-9822(95)00059-5 · Cited by 365
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Cited by
Structural Basis of Protein Kinase C Isoform Function
Steinberg, S. F. (2008) · Physiological Reviews · doi:10.1152/physrev.00034.2007 · Cited by 872
POWELL, D. J., TURBAN, S., GRAY, A., HAJDUCH, E., & HUNDAL, H. S. (2004) · Biochemical Journal · doi:10.1042/bj20040139 · Cited by 267
Dimopoulos, N., Watson, M., Sakamoto, K., & Hundal, H. S. (2006) · Biochemical Journal · doi:10.1042/bj20060244 · Cited by 247
Green, C. J., Henriksen, T. I., Pedersen, B. K., & Solomon, T. P. J. (2012) · PLoS ONE · doi:10.1371/journal.pone.0044284 · Cited by 80
Protein Kinase C Isoforms Have Differential Roles in the Regulation of Human Sebocyte Biology
Géczy, T., Oláh, A., Tóth, B. I., Czifra, G., Szöllősi, A. G., Szabó, T., Zouboulis, C. C., Paus, R., & Bíró, T. (2012) · Journal of Investigative Dermatology · doi:10.1038/jid.2012.94 · Cited by 20
Metadata
- Authors
- Alessi, D. R.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1997-01-27
- Volume
- 402
- Issue
- 2-3
- Pages
- 121-123
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2012051875
- Cited by
- 200
- References
- 1
- FWCI
- 5.40
- Type
- journal article
- Language
- en
- Open access
- closed
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- Alessi, D. R. (1997). The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase‐1β (Rsk‐2) and p70 S6 kinase. FEBS Letters. https://doi.org/10.1016/s0014-5793(96)01510-4
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
