The emerging role of lysine methyltransferase SETD8 in human diseases

SETD8/SET8/Pr-SET7/KMT5A is the only known lysine methyltransferase (KMT) that monomethylates lysine 20 of histone H4 (H4K20) in vivo. Lysine residues of non-histone proteins including proliferating cell nuclear antigen (PCNA) and p53 are also monomethylated. As a consequence, the methyltransferase...

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Autores principales: Milite, Ciro, Feoli, Alessandra, Viviano, Monica, Rescigno, Donatella, Cianciulli, Agostino, Balzano, Amodio Luca, Mai, Antonello, Castellano, Sabrina, Sbardella, Gianluca
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2016
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5034662/
https://www.ncbi.nlm.nih.gov/pubmed/27688818
http://dx.doi.org/10.1186/s13148-016-0268-4
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author Milite, Ciro
Feoli, Alessandra
Viviano, Monica
Rescigno, Donatella
Cianciulli, Agostino
Balzano, Amodio Luca
Mai, Antonello
Castellano, Sabrina
Sbardella, Gianluca
author_facet Milite, Ciro
Feoli, Alessandra
Viviano, Monica
Rescigno, Donatella
Cianciulli, Agostino
Balzano, Amodio Luca
Mai, Antonello
Castellano, Sabrina
Sbardella, Gianluca
author_sort Milite, Ciro
collection PubMed
description SETD8/SET8/Pr-SET7/KMT5A is the only known lysine methyltransferase (KMT) that monomethylates lysine 20 of histone H4 (H4K20) in vivo. Lysine residues of non-histone proteins including proliferating cell nuclear antigen (PCNA) and p53 are also monomethylated. As a consequence, the methyltransferase activity of the enzyme is implicated in many essential cellular processes including DNA replication, DNA damage response, transcription modulation, and cell cycle regulation. This review aims to provide an overview of the roles of SETD8 in physiological and pathological pathways and to discuss the progress made to date in inhibiting the activity of SETD8 by small molecules, with an emphasis on their discovery, selectivity over other methyltransferases and cellular activity.
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spelling pubmed-50346622016-09-29 The emerging role of lysine methyltransferase SETD8 in human diseases Milite, Ciro Feoli, Alessandra Viviano, Monica Rescigno, Donatella Cianciulli, Agostino Balzano, Amodio Luca Mai, Antonello Castellano, Sabrina Sbardella, Gianluca Clin Epigenetics Review SETD8/SET8/Pr-SET7/KMT5A is the only known lysine methyltransferase (KMT) that monomethylates lysine 20 of histone H4 (H4K20) in vivo. Lysine residues of non-histone proteins including proliferating cell nuclear antigen (PCNA) and p53 are also monomethylated. As a consequence, the methyltransferase activity of the enzyme is implicated in many essential cellular processes including DNA replication, DNA damage response, transcription modulation, and cell cycle regulation. This review aims to provide an overview of the roles of SETD8 in physiological and pathological pathways and to discuss the progress made to date in inhibiting the activity of SETD8 by small molecules, with an emphasis on their discovery, selectivity over other methyltransferases and cellular activity. BioMed Central 2016-09-22 /pmc/articles/PMC5034662/ /pubmed/27688818 http://dx.doi.org/10.1186/s13148-016-0268-4 Text en © The Author(s). 2016 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Review
Milite, Ciro
Feoli, Alessandra
Viviano, Monica
Rescigno, Donatella
Cianciulli, Agostino
Balzano, Amodio Luca
Mai, Antonello
Castellano, Sabrina
Sbardella, Gianluca
The emerging role of lysine methyltransferase SETD8 in human diseases
title The emerging role of lysine methyltransferase SETD8 in human diseases
title_full The emerging role of lysine methyltransferase SETD8 in human diseases
title_fullStr The emerging role of lysine methyltransferase SETD8 in human diseases
title_full_unstemmed The emerging role of lysine methyltransferase SETD8 in human diseases
title_short The emerging role of lysine methyltransferase SETD8 in human diseases
title_sort emerging role of lysine methyltransferase setd8 in human diseases
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5034662/
https://www.ncbi.nlm.nih.gov/pubmed/27688818
http://dx.doi.org/10.1186/s13148-016-0268-4
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