PAOA

PAOA is a selective histone deacetylase (HDAC) inhibitor with IC₅₀ values of 199 and 69 nM for HDAC1 and HDAC3, respectively.¹ It is selective for HDAC1 and HDAC3, having IC₅₀ values greater than 1.59 μM for HDAC2, 4, 5, 7, and 8 in a cell-free enzyme assay. In vitro, PAOA induces histone H3 and H4 hyperacetylation.² PAOA improves the metabolic deficit exhibited by murine striatal cells isolated from Hdh^Q111 knock-in mice in a dose-dependent manner and reduces eye neurodegeneration in a D. melanogaster model of Huntington’s disease.¹ In vivo, PAOA prevents formation of Huntingtin (Htt) protein aggregates in the brain and reduces the cognitive deficits in the N171-82Q mouse model of Huntington’s disease.³

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1. Jia, H., Pallos, J., Jacques, V., et al. Histone deacetylase (HDAC) inhibitors targeting HDAC3 and HDAC1 ameliorate polyglutamine-elicited phenotypes in model systems of Huntington’s disease. Neurobiol. Dis. 46(2), 351-361 (2012).

2. Mai, A., Perrone, A., Nebbioso, A., et al. Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: Histone deacetylase inhibition and in-cell activities. Bioorg. Med. Chem. Lett. 18(8), 2530-2535 (2008).

3. Jia, H., Kast, R.J., Steffan, J.S., et al. Selective histone deacetylase (HDAC) inhibition imparts beneficial effects in Huntington’s disease mice: Implications for the ubiquitin-proteasomal and autophagy systems. Hum. Mol. Genet. 21(24), 5280-5293 (2012).