The DOI matches its Crossref record; 25 of the 25 references it cites were found in a registry or an index.
Competitive inhibition by diacylglycerol of specific phorbol ester binding.
Open accessAbstract
Emerging evidence suggests that the phorbol ester receptor in brain may be the same as the Ca2+-phospholipid-dependent protein kinase (protein kinase C). Since protein kinase C activity is stimulated by unsaturated diacylglycerol and the phorbol esters can substitute for diacylglycerol in this stimulation, we have examined the effect of diacylglycerols on phorbol ester binding. Assays were carried out with the mouse brain cytosolic phorbol ester aporeceptor, which requires phospholipids for activity. In the presence of phosphatidylserine at 0.96 mg/ml, diolein inhibited specific binding of [3H]phorbol 12,13-dibutyrate ( [3H]PBt2) in a dose-dependent fashion to less than 10% of control levels. The inhibition curves fit the curve expected for a competitive inhibitor and yielded a Ki of 3.6 +/- 0.8 micrograms/ml (n = 5) [0.38% (wt/wt) the concentration of phosphatidylserine]. Scatchard analysis confirmed the competitive nature of the inhibition. At constant phospholipid concentrations, the Ki determined for diolein was independent of the diolein concentrations over the range of 1.5-80 micrograms/ml, suggesting that the inhibition did not arise simply by perturbation of the phospholipid bilayers. The Ki of diolein was approximately proportional to the absolute phospholipid concentration. With phosphatidylserine at 4.8 micrograms/ml, for example, the Ki was 52 ng/ml (1.1% of phosphatidylserine). In addition to diolein, the short-chain saturated diacylglycerol derivatives dicaprylin and dicaproin also inhibited [3H]PBt2 binding, whereas the long-chain saturated derivatives dipalmitin and distearin were much less active. Our results suggest (i) that diacylglycerol may act as an endogenous ligand for the phorbol ester receptor and (ii) that variation in lipid composition provides a mechanism for modulating phorbol ester receptor affinity.
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Inositol phospholipids and cell surface receptor function
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Phorbol diester receptor copurifies with protein kinase C.
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In vitro studies on the mode of action of the phorbol esters, potent tumor promoters: Part 1
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Self-citationTumor Promoters and the Mechanism of Tumor Promotion
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Cited by
Protein kinase C and other diacylglycerol effectors in cancer
Griner, E. M., & Kazanietz, M. G. (2007) · Nature Reviews Cancer · doi:10.1038/nrc2110 · Cited by 978
Cloning and expression of multiple protein kinase C cDNAs
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Munc13-1 is a presynaptic phorbol ester receptor that enhances neurotransmitter release
Betz, A., Ashery, U., Rickmann, M., Augustin, I., Neher, E., Südhof, T. C., Rettig, J., & Brose, N. (1998) · Neuron · doi:10.1016/s0896-6273(00)80520-6 · Cited by 425
Protein kinase C overactivity impairs prefrontal cortical regulation of working memory
Birnbaum, S. G., Yuan, P. X., Wang, M., Vijayraghavan, S., Bloom, A. K., Davis, D. J., Gobeske, K. T., Sweatt, J. D., Manji, H. K., & Arnsten, A. F. T. (2004) · Science · doi:10.1126/science.1100021 · Cited by 318
C1 domains exposed: From diacylglycerol binding to protein–protein interactions
COLONGONZALEZ, F., & KAZANIETZ, M. (2006) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2006.05.001 · Cited by 308
Metadata
- Authors
- Sharkey, N. A., Leach, K. L., & Blumberg, P. M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1984-01
- Volume
- 81
- Issue
- 2
- Pages
- 607-610
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1974638880
- Cited by
- 306
- References
- 25
- FWCI
- 12.63
- Type
- journal article
- Language
- en
- Open access
- green
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