Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

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Gompel M, Leost M, De Kier Joffe EB, Puricelli L, Franco LH, Palermo J, Meijer L

Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1703-7.

PubMed ID
15026054 [ View in PubMed
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Abstract

Meridianins are brominated 3-(2-aminopyrimidine)-indoles which are purified from Aplidium meridianum, an Ascidian from the South Atlantic (South Georgia Islands). We here show that meridianins inhibit various protein kinases such as cyclin-dependent kinases, glycogen synthase kinase-3, cyclic nucleotide-dependent kinases and casein kinase 1. Meridianins prevent cell proliferation and induce apoptosis, a demonstration of their ability to enter cells and to interfere with the activity of kinases important for cell division and cell death. These results suggest that meridianins constitute a promising scaffold from which more potent and selective protein kinase inhibitors could be designed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SeliciclibCyclin-dependent kinase 1IC 50 (nM)4507.230Details