Title : Differential effects of suramin on protein kinase C isoenzymes. A novel tool for discriminating protein kinase C activities.

Pub. Date : 1998 Jan 9

PMID : 9468299






9 Functional Relationships(s)
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1 Here we report on a differential effect of suramin on PKCmu and various PKC isoforms representing the cPKC, nPKC, and aPKC group of the PKC family. Suramin protein kinase C zeta Homo sapiens
2 In the absence of any cofactors suramin activates all PKC isoforms in the order of aPKCzeta >> PKCmu > cPKC, nPKCdelta. Suramin protein kinase C zeta Homo sapiens
3 As judged by the Vmax/KM ratios (0.5 for PKCmu and 2.2 for PKCzeta) the substrate syntide 2 is phosphorylated by suramin-activated PKCzeta around four times more effectively than by suramin-activated PKCmu. Suramin protein kinase C zeta Homo sapiens
4 As judged by the Vmax/KM ratios (0.5 for PKCmu and 2.2 for PKCzeta) the substrate syntide 2 is phosphorylated by suramin-activated PKCzeta around four times more effectively than by suramin-activated PKCmu. Suramin protein kinase C zeta Homo sapiens
5 As judged by the Vmax/KM ratios (0.5 for PKCmu and 2.2 for PKCzeta) the substrate syntide 2 is phosphorylated by suramin-activated PKCzeta around four times more effectively than by suramin-activated PKCmu. Suramin protein kinase C zeta Homo sapiens
6 Suramin-activated PKCmu behaves like that activated by phosphatidylserine and the phorbol ester TPA regarding autophosphorylation and differential inhibition by the PKC inhibitors Go 6976 and Go 6983. Suramin protein kinase C zeta Homo sapiens
7 In the presence of activating cofactors, such as phosphatidylserine and TPA or cholesterol sulfate (for PKCzeta), the activity of the aPKCzeta is further stimulated, PKCmu is not significantly affected, and the cPKCs and the nPKCdelta are strongly inhibited by suramin. Suramin protein kinase C zeta Homo sapiens
8 The differential action of suramin on PKC isoenzymes might play a role in some of its biological effects, as for instance inhibition of proliferation and tumor development. Suramin protein kinase C zeta Homo sapiens
9 Moreover, due to this property suramin will possibly be a valuable tool for discriminating the activities of PKC isoenzymes in vitro and in vivo. Suramin protein kinase C zeta Homo sapiens