Cellular uptake and localization of fluorescent derivatives of phorbol ester tumor promoters

Liskamp, R.M., Brothman, A.R., Arcoleo, J.P., Miller, O.J. and Weinstein, I.B. (1985) Cellular uptake and localization of fluorescent derivatives of phorbol ester tumor promoters. Biochemical and Biophysical Research Communications, 131(2), pp. 920-927. (doi:10.1016/0006-291X(85)91327-0)

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Abstract

The synthetic fluorescent derivatives of 12-O-tetradecanoylphorbol-13-acetate (TPA), dansyl-TPA, dansyl-TPA-20-acetate and dansyl-TPA-13-desacetate, have ID50 values in the [3H]PDBu binding assay of 2nM, 30nM and 1000nM respectively; the ID50 value of TPA is 4nM. Dansyl-TPA is also equipotent with TPA as an activator of protein kinase C(PKC) producing half maximum stimulation at 2nM. Dansyl-TPA-13-desacetate is almost as potent as dansyl-TPA, while dansyl-TPA-20-acetate is completely inactive as an activator of PKC. The cellular uptake of these fluorescent TPA derivatives tends to parallel their activity in the [3H]PDBu binding assay. Treatment of C3H 10T1/2 cells with 100nM dansyl-TPA results in intense fluorescence of the entire cytoplasm, while the nucleus is virtually devoid of fluorescence. The uptake of fluorescence is quenched by an excess of TPA. Thus, dansyl-TPA rapidly enters cells and binds to specific sites distributed throughout the cytoplasm. Presumably these sites reflect the cellular localization of phorbol ester receptors and protein kinase C.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: Liskamp, R.M., Brothman, A.R., Arcoleo, J.P., Miller, O.J., and Weinstein, I.B.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Biochemical and Biophysical Research Communications
ISSN:0006-291X
ISSN (Online):1090-2104

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