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Updated: Jun 13, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids
Marc Lamblin1, Basel Dabbas, Russell Spingarn
1Department of Chemistry, McGill University, Montreal, QC, Canada.
Abstract:
Incorporation of zinc-binding groups into the side-chain of 1alpha,25-dihydroxyvitamin D(3) (1,25D) fully bifunctional hybrid molecules which act both as vitamin D receptor agonists and histone deacetylase inhibitors. These bifunctional hybrids display in vitro antiproliferative activity against the AT84 squamous carcinoma cell line while lacking the in vivo hypercalcemic effects of 1,25D.
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