Related Experiment Video
Updated: May 12, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
A small molecule inhibitor of fungal histone acetyltransferase Rtt109
Jessica Lopes da Rosa1, Vineeta Bajaj, James Spoonamore
1Program in Gene Function and Expression, Program in Molecular Medicine, University of Massachusetts Medical School, 364 Plantation St., LRB506, Worcester, MA 01605, USA.
Abstract:
The histone acetyltransferase Rtt109 is the sole enzyme responsible for acetylation of histone H3 lysine 56 (H3K56) in fungal organisms. Loss of Rtt109 renders fungal cells extremely sensitive to genotoxic agents, and prevents pathogenesis in several clinically important species. Here, via a high throughput chemical screen of >300,000 compounds, we discovered a chemical inhibitor of Rtt109 that does not inhibit other acetyltransferase enzymes. This compound inhibits Rtt109 regardless of which histone chaperone cofactor protein (Asf1 or Vps75) is present, and appears to inhibit Rtt109 via a tight-binding, uncompetitive mechanism.
More Related Videos
Related Concept Videos
Antifungal Agents
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a DNA...
Experimental RNAi
Inhibitors of Viral Protein Synthesis
Riboswitches
The aptamer has high specificity for a particular metabolite which allows riboswitches to specifically regulate...
Inhibitors of Bacterial Protein Synthesis

