title: An organometallic inhibitor for glycogen synthase kinase 3.
abstract: Replacing natural products with kinetically inert metal complexes may lead to a new class of therapeutics in which a metal center plays the role of an innocent bystander, organizing the orientation of the organic ligands in the receptor space. As an example of this approach, a ruthenium complex is described that copies the binding mode of indolocarbazole protein kinase inhibitors and serves as a reversible, low-nanomolar inhibitor for glycogen synthase kinase 3 (GSK-3).
authors.affiliation: Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104, USA.
authors.forename: Howard
authors.initials: H
authors.lastname: Bregman
authors.forename: Douglas S
authors.initials: DS
authors.lastname: Williams
authors.forename: G Ekin
authors.initials: GE
authors.lastname: Atilla
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Carroll
authors.forename: Eric
authors.initials: E
authors.lastname: Meggers
mesh_terms: D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D009942:Organometallic Compounds / Q000737:chemistry / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002227:Carbazoles; D007211:Indoles; D009942:Organometallic Compounds; D047428:Protein Kinase Inhibitors; D012428:Ruthenium; D038362:Glycogen Synthase Kinase 3