title: Development of a chimeric c-Src kinase and HDAC inhibitor.
abstract: On the basis of synergism observed between a selective c-Src kinase inhibitor with an HDAC inhibitor, the development of the first chimeric c-Src kinase and HDAC inhibitor is described. The optimized chimeric inhibitor is shown to be a potent c-Src and HDAC inhibitor. Chimeric inhibitor4is further shown to be highly efficacious in cancer cell lines and significantly more efficacious than a dual-targeting strategy using discrete c-Src and HDAC inhibitors.
authors.affiliation: Department of Chemistry, University of Michigan, 930 N. University Avenue, Ann Arbor, Michigan 48109, United States.
authors.forename: Kristin S
authors.initials: KS
authors.lastname: Ko
authors.forename: Michael E
authors.initials: ME
authors.lastname: Steffey
authors.forename: Kristoffer R
authors.initials: KR
authors.lastname: Brandvold
authors.forename: Matthew B
authors.initials: MB
authors.lastname: Soellner
keywords: HDAC; c-Src; chimera; combination therapy; kinase