Closer to class IIa HDAC inhibitors

GlaxoSmithKline plc and its Tempero Pharmaceuticals Inc. spinout have identified selective, first-in-class compounds that bind and inhibit the catalytic domain of class IIa histone deacetylases,1 a not-so-well-understood subset of the target family that has been genetically linked to several diseases.

Both companies initially plan to study the trifluoromethyloxadiazole (TFMO) molecules in autoimmune disease.

There are four distinct classes of histone deacetylases (HDACs), which are classified according to primary structure: class I (HDAC1, HDAC2, HDAC3 and HDAC8); class II, which is broken down into

class IIa (HDAC4, HDAC5, HDAC7 and HDAC9) and class IIb (HDAC6 and HDAC10); class III (sirtuin 1 (SIRT1)-SIRT7); and class IV (HDAC11).

Little is known about the specific cellular and biological functions of each class outside of class I. The difficulty in teasing out that information is exacerbated by the fact that few class-specific HDAC inhibitors exist.

At least 23 companies have HDAC

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