The Use of Nucleosome Substrates Improves Binding of SAM Analogs to SETD8

In this report, we present the development of a mechanistically balanced biochemical assay using full-length SETD8 and a recombinant nucleosome substrate. This improves the binding of SAM, SAH, and sinefungin by up to 10,000-fold. A small collection of inhibitors structurally related to SAM were screened and 40 compounds were identified that only inhibit SETD8 when a nucleosome substrate is used.
Source: Journal of Biomolecular Screening - Category: Molecular Biology Authors: Tags: Original Research Source Type: research