2 research outputs found
A Continuous, Fluorogenic Sirtuin 2 Deacylase Assay: Substrate Screening and Inhibitor Evaluation
Sirtuins are important regulators
of lysine acylation, which is implicated in cellular metabolism and
transcriptional control. This makes the sirtuin class of enzymes interesting
targets for development of small molecule probes with pharmaceutical
potential. To achieve detailed profiling and kinetic insight regarding
sirtuin inhibitors, it is important to have access to efficient assays.
In this work, we report readily synthesized fluorogenic substrates
enabling enzyme-economical evaluation of SIRT2 inhibitors in a continuous
assay format as well as evaluation of the properties of SIRT2 as a
long chain deacylase enzyme. Novel enzymatic activities of SIRT2 were
thus established in vitro, which warrant further investigation, and
two known inhibitors, suramin and SirReal2, were profiled against
substrates containing ε-<i>N</i>-acyllysine modifications
of varying length
Correction to A Continuous, Fluorogenic Sirtuin 2 Deacylase Assay: Substrate Screening and Inhibitor Evaluation
Correction to A
Continuous, Fluorogenic Sirtuin 2 Deacylase Assay: Substrate Screening
and Inhibitor Evaluatio