2oi4
Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole
OverviewOverview
A general route to ruthenium pyridocarbazole half-sandwich complexes is presented and applied to the synthesis of sixteen new compounds, many of which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into the pyridine moiety increases the binding affinity for glycogen synthase kinase 3 by almost one order of magnitude. These data are supplemented with cyclic voltammetry experiments and a protein co-crystallographic study.
About this StructureAbout this Structure
2OI4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand., Pagano N, Maksimoska J, Bregman H, Williams DS, Webster RD, Xue F, Meggers E, Org Biomol Chem. 2007 Apr 21;5(8):1218-27. Epub 2007 Mar 20. PMID:17406720 Page seeded by OCA on Sun May 4 10:58:22 2008