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Updated: Jan 26, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Novel squalene-hopene cyclase inhibitors derived from hydroxycoumarins and hydroxyacetophenones
Giancarlo Cravotto1, Gianni Balliano, Silvia Tagliapietra
1Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Torino, Italy. giancarlo.cravotto@unito.it
Abstract:
Squalene-hopene cyclase (SHC) is a useful model enzyme for predicting molecular interactions with oxidosqualene cyclase (OSC). Structure--activity relationships were investigated for numerous coumarin-derived inhibitors of SHC, and structural simplifications are suggested. Both umbelliferone and 2,4-dihydroxyacetophenone provide convenient starting nuclei for the design of SHC inhibitors. Derivatives bearing an omega-epoxyfarnesyl moiety or just a plain alkyl chain showed an inhibitory effect on a recombinant SHC from Alicyclobacillus acidocaldarius expressed in Escherichia coli.
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