Benzyl and phenethyl isothiocyanates as promising epigenetic drug compounds by modulating histone acetylation and methylation marks in malignant melanoma

Summary Melanoma is an aggressive skin cancer with increasing incidence rates globally. On the other hand, isothiocyanates are derived from cruciferous vegetables and are known to exert a wide range of anti-cancer activities including, among others, their ability to interact with the epigenome in or...

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Veröffentlicht in:Investigational new drugs 2021-12, Vol.39 (6), p.1460-1468
Hauptverfasser: Mitsiogianni, Melina, Anestopoulos, Ioannis, Kyriakou, Sotiris, Trafalis, Dimitrios T., Franco, Rodrigo, Pappa, Aglaia, Panayiotidis, Mihalis I.
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container_end_page 1468
container_issue 6
container_start_page 1460
container_title Investigational new drugs
container_volume 39
creator Mitsiogianni, Melina
Anestopoulos, Ioannis
Kyriakou, Sotiris
Trafalis, Dimitrios T.
Franco, Rodrigo
Pappa, Aglaia
Panayiotidis, Mihalis I.
description Summary Melanoma is an aggressive skin cancer with increasing incidence rates globally. On the other hand, isothiocyanates are derived from cruciferous vegetables and are known to exert a wide range of anti-cancer activities including, among others, their ability to interact with the epigenome in order to supress cancer progression. The aim of this study was to determine the role of phenethyl and benzyl isothiocyanates in modulating histone acetylation and methylation as a potential epigenetic therapeutic strategy in an in vitro model of malignant melanoma. We report that both isothiocyanates induced cytotoxicity and influenced acetylation and methylation status of specific lysine residues on histones H3 and H4 by modulating the expression of various histone acetyltransferases, deacetylases and methyltransferases in malignant melanoma cells. Our data highlight novel insights on the interaction of isothiocyanates with components of the histone regulatory machinery in order to exert their anti-cancer action in malignant melanoma.
doi_str_mv 10.1007/s10637-021-01127-0
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On the other hand, isothiocyanates are derived from cruciferous vegetables and are known to exert a wide range of anti-cancer activities including, among others, their ability to interact with the epigenome in order to supress cancer progression. The aim of this study was to determine the role of phenethyl and benzyl isothiocyanates in modulating histone acetylation and methylation as a potential epigenetic therapeutic strategy in an in vitro model of malignant melanoma. We report that both isothiocyanates induced cytotoxicity and influenced acetylation and methylation status of specific lysine residues on histones H3 and H4 by modulating the expression of various histone acetyltransferases, deacetylases and methyltransferases in malignant melanoma cells. 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subjects Acetylation
Acetylation - drug effects
Anticancer properties
Cell Line, Tumor
Cell Survival
Cytotoxicity
Epigenesis, Genetic
Epigenetics
Histones
Histones - drug effects
Humans
Isothiocyanates - pharmacology
Lysine
Medicine
Medicine & Public Health
Melanoma
Melanoma - physiopathology
Methylation
Methylation - drug effects
Oncology
Pharmacology/Toxicology
Preclinical Studies
Skin cancer
Skin Neoplasms - physiopathology
Toxicity
title Benzyl and phenethyl isothiocyanates as promising epigenetic drug compounds by modulating histone acetylation and methylation marks in malignant melanoma
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