Rapid Screening Assay for Novel Epigenetic Drugs

DESCRIPTION (provided by applicant): A hallmark of virtually every cancer is aberrant epigenetic silencing of vital genes required for a normal cell cycle and genome stability (e.g. MLH1, BRCA1, VHL, p16, etc.). Loss of expression of these tumor suppressorgenes plays a critical role in cancer formation and growth. Thus, targeting this root cause of cancer has significant potential to treat and potentially cure a host of cancers. Indeed, a major initiative i essentially every major pharmaceutical company isto investigate epigenetic cancer therapies targeting the reactivation of these key genes. However, despite its promise, at this time drug-induced gene reactivation does not work therapeutically because reactivation is invariably unstable. One reason for this failure is that current approaches consider silencing as an end point instead of a process, and as a result do not strategically target epigenetic modifications that occur at different times during the silencing process. We believe achieving stabl