This project has discovered and developed a novel chemotype for the potential treatment of cancer. The studies underway have elucidated some of the key chemical structure necessary for the observed activity and further studies are underway to fully delineate the structure activity relationships of this class of molecules. The development of these molecules is underway to advance from the initial hit into a lead structure for treatment development. Samples have been submitted to the NCI60 screen and some have advanced to hollow fiber testing. Additionally the core has facilitated the preparation of other biological probes for the study biologically relevant processes. Projects collaboratively supported by the core facility include: Z01 DK036136-03 -- The deubiquitinating inhibitor EerI induces tumor cell apoptosis Z01 AR041099-18 -- Genetic Metabolic Myopathies--phosphofructokinase/acid Maltase Deficiency Z01 AR041165-02 -- Role of Skeletal Muscle SIRT1 in the Pathogenesis of Metabolic Disorders Z01 DK031143-05 -- Chemically Modified Peptide Nucleic Acids
| Wang, Qiuyan; Mora-Jensen, Helena; Weniger, Marc A et al. (2009) ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc Natl Acad Sci U S A 106:2200-5 |
