An organometallic inhibitor for glycogen synthase kinase 3

Howard Bregman; Douglas S Williams; G Ekin Atilla; Patrick J Carroll; Eric Meggers

doi:10.1021/ja046049c

An organometallic inhibitor for glycogen synthase kinase 3

J Am Chem Soc. 2004 Oct 27;126(42):13594-5. doi: 10.1021/ja046049c.

Authors

Howard Bregman¹, Douglas S Williams, G Ekin Atilla, Patrick J Carroll, Eric Meggers

Affiliation

¹ Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104, USA.

PMID: 15493898
DOI: 10.1021/ja046049c

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Carbazoles / chemistry
Carbazoles / pharmacology
Crystallography, X-Ray
Glycogen Synthase Kinase 3 / antagonists & inhibitors*
Glycogen Synthase Kinase 3 / metabolism
Indoles / chemistry
Indoles / pharmacology
Kinetics
Models, Molecular
Organometallic Compounds / chemistry
Organometallic Compounds / pharmacology*
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology*
Ruthenium / chemistry
Ruthenium / pharmacology*

Substances

Carbazoles
Indoles
Organometallic Compounds
Protein Kinase Inhibitors
Ruthenium
Glycogen Synthase Kinase 3