Development of a NanoBRET assay to validate inhibitors of Sirt2-mediated lysine deacetylation and defatty-acylation that block prostate cancer cell migration

Vogelmann A, Schiedel M, Wössner N, Merz A, Herp D, Hammelmann S, Colcerasa A, Komaniecki G, Hong JY, Sum M, Metzger E, Neuwirt E, Zhang L, Einsle O, Groß O, Schüle R, Lin H, Sippl W, Jung M.

RSC Chem Biol. 2022; doi: 10.1039/d1cb00244a.

We present new inhibitors for the NAD+-dependent lysine deacetylase and defatty-acylase Sirtuin2 (Sirt2) that block migration and downregulate c-Myc protein levels in prostate cancer cells. Furthermore, we developed a NanoBRET assay to validate cellular target engagement of Sirt2 inhibitors.

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