Design and Application of Cofactor Analogues as Chemical Tools to Probe Lysine Acetyltransferase Ligands Targeting the Catalytic Domain

03 December 2018, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


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.


histone acetyltransferases
Histone Acetyltransferase hMOF
Cofactors (biochemistry)
p300/CBP associated factor

Supplementary materials

Supporting Information 181128


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