TR-FRET Assay for Sirtuin 1 (SIRT1) Inhibitor Screening
Abstract
SIRT1 is an enzyme from the sirtuin family. Sirtuins are NAD<sup>+</sup>-dependent protein deacetylases. This enzyme family is responsible in pathways involved in apoptosis, cellular stress, and aging. Theories have been set forth regarding SIRT1 biochemical pathway, but no exact mechanism is known. Screening for potential modulators of this enzyme can lead the way to uncovering the sirtuin deacetylase mechanism and finding possible compounds as candidates for drugs in treating cancer and metabolic diseases. Known inhibitors and potential inhibitors were screened using a SIRT1 assay adapted from Cisbio. We were able to validate known inhibitors through dose curves and set assay parameters through titration experiments z > 0.5. With regards to potential inhibitors, there are preliminary results indicating some inhibitory effects.