| Specificity and mechanism of protein kinase C activation by sn-1,2-diacylglycerols. | |
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MedLine Citation:
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PMID: 3456578 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The specificity of protein kinase C activation by sn-1,2-diacylglycerols and analogues was investigated by using a Triton X-100 mixed micellar assay [Hannun, Y. A., Loomis, C. R. & Bell, R. M. (1985) J. Biol. Chem. 260, 10039-10043]. Analogues containing acyl or alkyl chains eight carbons in length were synthesized because sn-1,2-dioctanoylglycerol is an effective cell-permeant activator of protein kinase C. These analogues were tested as activators and antagonists of rat brain protein kinase C to determine the exact structural features important for activity. The analogues established that activation of protein kinase C by diacylglycerols is highly specific. Several analogues established that both carbonyl moieties of the oxygen esters are required for maximal activity and that the 3-hydroxyl moiety is also required. None of the analogues were antagonists. These data, combined with previous investigations, permitted formulation of a model of protein kinase C activation. A three-point attachment of sn-1,2-diacylglycerol to the surface-bound protein kinase C-phosphatidylserine-Ca2+ complex is envisioned to cause activation. Direct ligation of diacylglycerol to Ca2+ is proposed to be an essential step in the mechanism of activation of protein kinase C. |
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Authors:
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B R Ganong; C R Loomis; Y A Hannun; R M Bell |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Proceedings of the National Academy of Sciences of the United States of America Volume: 83 ISSN: 0027-8424 ISO Abbreviation: Proc. Natl. Acad. Sci. U.S.A. Publication Date: 1986 Mar |
Date Detail:
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Created Date: 1986-04-10 Completed Date: 1986-04-10 Revised Date: 2009-11-18 |
Medline Journal Info:
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Nlm Unique ID: 7505876 Medline TA: Proc Natl Acad Sci U S A Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1184-8 Citation Subset: IM |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Brain / enzymology Diglycerides / pharmacology* Enzyme Activation / drug effects Glycerides / pharmacology* Micelles Models, Molecular Protein Kinase C / metabolism* Rats Structure-Activity Relationship |
| Grant Support | |
ID/Acronym/Agency:
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AM20205/AM/NIADDK NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Diglycerides; 0/Glycerides; 0/Micelles; EC 2.7.11.13/Protein Kinase C |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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