Inhibitors selective for HDAC6 in enzymes and cells.

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Gupta PK, Reid RC, Liu L, Lucke AJ, Broomfield SA, Andrews MR, Sweet MJ, Fairlie DP

Inhibitors selective for HDAC6 in enzymes and cells.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. doi: 10.1016/j.bmcl.2010.09.100. Epub 2010 Oct 12.

PubMed ID

20947351 [ View in PubMed

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Abstract

Histone deacetylase inhibitors with anticancer or anti-inflammatory activity bind to Class I or Class I and II HDAC enzymes. Here we compare selectivity of inhibitors of a Class II HDAC enzyme (HDAC6) and find one that retains high selectivity in macrophages.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Vorinostat	Histone deacetylase 1	IC 50 (nM)	76	N/A	N/A	Details
Vorinostat	Histone deacetylase 6	IC 50 (nM)	85	N/A	N/A	Details