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Updated: Nov 21, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Antibody drug conjugates with hydroxamic acid cargos for histone deacetylase (HDAC) inhibition
Claudio Cianferotti1, Valentina Faltoni1, Elena Cini1
1Dipartimento di Biotecnologie, Chimica e Farmacia, Università di Siena, Via A. Moro 2, 53100 Siena, Italy. maurizio.taddei@unisi.it.
Abstract:
Antitumor hydroxamates SAHA and Dacinostat have been linked to cetuximab and trastuzumab through a non-cleavable linker based on the p-mercaptobenzyl alcohol structure. These antibody drug conjugates (ADCs) were able to inhibit HDAC in several tumour cell lines. The cetuximab based ADCs block human lung adenocarcinoma cell proliferation, demonstrating that bioconjugation with antibodies is a suitable approach for targeted therapy based on hydroxamic acid-containing drugs. This work also shows that ADC-based delivery might be used to overcome the classical pharmacokinetic problems of hydroxamic acids.
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