Histone deacetylases (HDACs) are key components of the epigenetic machinery controlling gene expression. They are involved in chromatin remodeling events via post-translational histone modifications but may also act on nonhistone proteins, influencing many fundamental cellular processes. Due to the key involvement of HDACs in serious human pathologies, including cancer, HDAC inhibitors (HDACis) have received increased attention in recent years. It is known that marine invertebrates produce significant amounts of secondary metabolites showing active pharmacological properties and an extensive spectrum of biomedical applications. The aim of this review is to gather selected studies that report the extraction and identification of marine invertebrate-derived compounds that possess HDACi properties, grouping the producing species according to their taxonomic hierarchy. The molecular, biochemical, and/or physiological aspects, where available, and modes of action of these naturally occurring HDACis will be recapitulated, taking into consideration their possible utilization for the future design of analogs with increased bioavailability and efficacy, less toxicity, and, also, higher isoform selectivity.

Luparello, C., Mauro, M., Arizza, V., Vazzana, M. (2020). Histone Deacetylase Inhibitors from Marine Invertebrates. BIOLOGY, 9(12), 1-24 [10.3390/biology9120429].

Histone Deacetylase Inhibitors from Marine Invertebrates

Luparello, Claudio
;
Mauro, Manuela;Arizza, Vincenzo;Vazzana, Mirella
2020-01-01

Abstract

Histone deacetylases (HDACs) are key components of the epigenetic machinery controlling gene expression. They are involved in chromatin remodeling events via post-translational histone modifications but may also act on nonhistone proteins, influencing many fundamental cellular processes. Due to the key involvement of HDACs in serious human pathologies, including cancer, HDAC inhibitors (HDACis) have received increased attention in recent years. It is known that marine invertebrates produce significant amounts of secondary metabolites showing active pharmacological properties and an extensive spectrum of biomedical applications. The aim of this review is to gather selected studies that report the extraction and identification of marine invertebrate-derived compounds that possess HDACi properties, grouping the producing species according to their taxonomic hierarchy. The molecular, biochemical, and/or physiological aspects, where available, and modes of action of these naturally occurring HDACis will be recapitulated, taking into consideration their possible utilization for the future design of analogs with increased bioavailability and efficacy, less toxicity, and, also, higher isoform selectivity.
Settore BIO/06 - Anatomia Comparata E Citologia
Settore BIO/05 - Zoologia
Luparello, C., Mauro, M., Arizza, V., Vazzana, M. (2020). Histone Deacetylase Inhibitors from Marine Invertebrates. BIOLOGY, 9(12), 1-24 [10.3390/biology9120429].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/444996
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