MG149 is cell-permeable anacardic acid analog that displays higher selectivity towards MYST type HATs (IC50 = 47 and 74 μM against MOF and Tip60; Ki for KAT8 = 39 μM) over p300 and PCAF (IC50 > 200 and >> 200 uM). Tip60 inhibition is shown to be Ac-CoA competitive and histone substrate non-competitive and KAT8 inhibition is Ac-CoA uncompetitive. MG149 treatment lowers histone acetylation levels and cellular proliferation rate, induces apoptosis and dose-dependently alters pro-inflammatory cytokines/chemokines expression. Enhances JQ1-induced HIV latency reversal, suppresses NOX transcription and ameliorates ROS levels.
cell-permeable anacardic acid analog that displays higher selectivity towards MYST type HATs over p300 and PCAF
Excessive accumulation of reactive oxygen species (ROS), catalyzed by the NADPH oxidases (NOX), is involved in the pathogenesis of ischemia-reperfusion (IR) injury. The underlying epigenetic mechanism remains elusive. We evaluated the potential role of megakaryocytic leukemia 1 (MKL1), as a
European journal of medicinal chemistry, 47(1), 337-344 (2011-11-22)
Histone acetyltransferases are important enzymes that regulate various cellular functions, such as epigenetic control of DNA transcription. Development of HAT inhibitors with high selectivity and potency will provide powerful mechanistic tools for the elucidation of the biological functions of HATs
Lysine acetylations are post-translational modifications of cellular proteins, that are crucial in the regulation of many cellular processes. Lysine acetylations on histone proteins are part of the epigenetic code regulating gene expression and are installed by histone acetyltransferases. Observations that
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