BMC Chemical Biology - Latest articlesThe latest articles from BMC Chemical Biology (ISSN 1472-6769) published by BioMed CentralSmall-molecule and mutational analysis of allosteric Eg5 inhibition by monastrol- February 27, 2006 Background: A recent crystal structure of monastrol in a ternary complex with the kinesin Eg5 motor domain highlights a novel, induced-fit drug binding site at atomic resolution. Mutational obliteration of the monastrol binding site results in a monastrol-resistant, but otherwise catalytically active Eg5 motor domain. However, considering the conformational changes at this site, it is unclear what specific interactions stabilize the interaction between monastrol and the Eg5 motor...http://www.biomedcentral.com/1472-6769/6/2 Uncharged isocoumarin-based inhibitors of urokinase-type plasminogen activator- February 8, 2006 Background: Urokinase-type plasminogen activator (uPA) plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis. Consequently, uPA is an attractive target for the development of small molecule active site inhibitors. Most of the recent drug development programs aimed at nonpeptidic inhibitors targeted at uPA have focused on arginino mimetics containing amidine or guanidine functional groups attached to aromatic or heterocyclic...http://www.biomedcentral.com/1472-6769/6/1 |