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. doi: 10.1016/j.bmcl.2004.01.050.
- 1. C.N.R.S., Cell Cycle Group, Station Biologique, B.P. 74, 29682 Roscoff cedex, Bretagne, France.
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.