New preprint 🧵 Class IV sirtuins SIRT6/SIRT7 only work on nucleosomes, and peptide assays fail.
We engineered a fluorescent reporter into semi-synthetic nucleosomes: real-time kinetics, nanomolar Km, Z' >0.8 - and found a selective SIRT6 inhibitor.
chemrxiv.org/doi/full/10.26…
chemrxiv.org A Fluorescent Nucleosome Platform for High-Throughput Sirtuin Kinetic Analysis and Inhibitor... The class IV sirtuins SIRT6 and SIRT7 are epigenetic protein lysine deacylases identified as targets for cancer treatment, including pancreatic ductal adenocarcinoma (PDAC). However, small molecules... We engineered a fluorescent reporter into semi-synthetic nucleosomes: real-time kinetics, nanomolar Km, Z' >0.8 - and found a selective SIRT6 inhibitor.
chemrxiv.org/doi/full/10.26…
