SIRT6 or Sirtuin 6 proteins are a class of proteins that possess either histone deacetylase or mono-ribosyltransferase activity. SIRT6 is a nuclear sirtuin that has been associated with aging, cellular protection, sugar metabolism and certain types of cancer. Broad therapeutic applications are foreseen for SIRT6 inhibitors, including uses in diabetes, immune-mediated disorders, and cancer. Unlike other known protein deacetylases, which simply hydrolyze acetyl-lysine residues, the sirtuin-mediated deacetylation reaction hydrolyzes acetyl-lysine and NAD. This hydrolysis yields the deacetylated substrate, O-acetyl-ADP-ribose and nicotinamide, itself an inhibitor of sirtuin activity. Studies suggest that the human sirtuins may function as intracellular regulatory proteins with mono-ADP-ribosyltransferase activity.
Features and Benefits
Compatible with high-throughput handling systems.
Suitability
Suitable for screening, characterizing and studying SIRT6 inhibitors
Principle
In this Sirtuin 6 inhibitor screening kit, Sirtuin 6 deacetylates the substrate, followed by cleavage of the deacetylated substrate to release the fluorescent group, which is detected fluorometrically (λex = 400 nm/λem = 505 nm).
Proceedings of the National Academy of Sciences of the USA, 107, 21790-21794 (2010)
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