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Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor
It is shown that activation of the canonical Wnt pathway is sufficient to maintain self-renewal of both HESCs and MESCs, and the use of GSK-3-specific inhibitors such as BIO may have practical applications in regenerative medicine.
Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5.
Through its unique selectivity for some cyclin-dependent kinases, roscovitine provides a useful antimitotic reagent for cell cycle studies and may prove interesting to control cells with deregulated cdc2, cdk2 or cdk5 kinase activities.
GSK-3-selective inhibitors derived from Tyrian purple indirubins.
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases
Indirubin-3′-monoxime inhibits the proliferation of a large range of cells, mainly through arresting the cells in the G2/M phase of the cell cycle, which has implications for therapeutic optimization of indigoids.
Phosphorylation of DARPP-32 by Cdk5 modulates dopamine signalling in neurons
Dopamine and cyclic AMP-regulated phospho-protein DARPP-32 is a bifunctional signal transduction molecule which, by distinct mechanisms, controls a serine/threonine kinase and aserine/Threonine phosphatase.
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase…
- S. Leclerc, M. Garnier, L. Meijer
- Biology, ChemistryThe Journal of biological chemistry
- 5 January 2001
It is reported here that indirubins are also powerful inhibitors (IC(50): 5-50 nm) of an evolutionarily related kinase, glycogen synthase kinase-3beta (GSK-3 beta), and it is shown that many, but not all, reported CDK inhibitors are powerful inhibitors of GSK-3 Beta.
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
Purine libraries could provide useful tools for analyzing a variety of signaling and regulatory pathways and may lead to the development of new therapeutics.
Pharmacological inhibitors of glycogen synthase kinase 3.
Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine.
- W. F. De Azevedo, S. Leclerc, L. Meijer, L. Havlícek, M. Strnad, S. Kim
- Chemistry, BiologyEuropean journal of biochemistry
- 15 January 1997
Results from structure/activity studies and from analysis of the cdk2/roscovitine complex crystal structure should allow the design of even more potent cdk inhibitors.