Gabriela Vilema-Enríquez, Robert Quinlan, Peter Kilfeather, Roberta Mazzone, Saba Saqlain, Irene del Molino del Barrio, Annalidia Donato, Gabriele Corda, Fengling Li, Masoud Vedadi, Andrea H Németh, Paul E Brennan, Richard Wade-Martins; bioRxiv 2020.03.26.010439; doi:10.1101/2020.03.26.010439
Finally, based on the structural activity relationship and crystal structure of A-196, novel small molecule A-196 analogues were synthesized and shown to give a 20-fold increase in potency for increasing FXN expression. Overall, our results suggest that histone methylation is important in the regulation of FXN expression, and highlight SUV4-20 H1 as a potential novel therapeutic target for FRDA.
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