SIRT5 is a mitochondrial and cytoplasmic enzyme that is found in the histone deacetylase (HDAC) family.  The role of a HDAC enzyme is to take acetyl groups off of histones and other molecules within the cell as a means of regulation.  As class three HDAC enzymes, SIRT5 and its fellow sirtuin proteins are metal-independent histone deacetylases.  SIRT5 has been proven to function more effectively as a desuccinylase and demalonylase. It has been previously determined that whilst inhibitors or activators of the sirtuin sub-family are rare, derivatives of barbiturate groups have been successful as starting points for further optimization.  The study here shows the analysis of an in-house library of nearly 400 compounds by way of a spectrofluorometric trypsin coupled assay system for potential therapeutic bases for drug design.  Two barbiturate derivatives, MDS 3-16 and MH 5-75, showed an inhibitory effect each of 30%.

Discovery of novel inhibitors for the SIRT5 enzyme

247th National Meeting (2014)

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