Biological and Medicinal Chemistry

Cofactor Analogues as Active Site Probes in Lysine Acetyltransferases



Here we present the synthesis of two functional cofactor-based chemical probes and their usage as mechanistic tools in a broadly applica-ble assay platform for histone acetyltransferases (HATs). In this platform, a fluorescence polarization (FP) based binding assay was combined with biolayer interferometry (BLI) competition analysis and a FP competition activity immunoassay to enable easy, reliable, and pro-found evaluation of ligands that target the KAT cofactor binding site.

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2.0 revised prepint


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Supplementary material

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Supporting Information for Publication