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Updated: Oct 9, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin.
S L Colletti1, R W Myers, S J Darkin-Rattray
1Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065, USA. steve_colletti@merck.com
Abstract:
Apicidin, a natural product recently isolated at Merck, inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nanomolar inhibitor of HDACs, into a series of side-chain analogues that display picomolar enzyme affinity is described within this structure-activity study.
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