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söndag 16 november 2025

Sirt2 (Sirtuiineista jatkoa: Sirtuiini 2;n osuudesta epigeneettisessä säätelyssä. Sirtuiini 2. Kesken)

https://febs.onlinelibrary.wiley.com/doi/10.1111/febs.13053

Review Article
Free Access

Sirtuin-dependent epigenetic regulation in the maintenance of genome integrity

First published: 15 September 2014
Citations: 110

Abstract

Sirtuins are a family of deacetylases that target histone and non-histone proteins and require NAD+ as an enzymatic cofactor for their enzymatic activity. This requirement confers sirtuins with the ability to detect changes in metabolism and energy homeostasis and to coordinate cellular responses to maintain genome integrity. Thus, sirtuins are crucial in the crosstalk between environment and genome, and therefore in responses to stress at the cell and organism levels. Sirtuins play a major role in maintaining genome integrity, largely through regulation of epigenetic mechanisms. They target different histone marks, including H4K16Ac, H3K9Ac, H3K56Ac and H3K18Ac, and non-histone components of the chromatin machinery, such as enzymes and structural proteins. Here we summarize our current view on the link between sirtuins and epigenetics, one that reflects the continual adaptation of the genome to stress.

ERITYISETI SIRT2: 

SIRT2 Vaikka SIRT2 on pääasiassa lokalisoitunut sytoplasmaan, se pystyy deasetyloimaan H4K16Ac ja vähemmässä määrin myös H3K9Ac. RNA-interferenssitutkimuksin on osoitettu, että SIRT2:n kato korreloi korkeisiin H4K16Ac:n pitoisuuksiin, mikä on analogista SIRT1:n kadon kanssa. Tämä SIRT2-aktiivisuus on evoluution aikana konservoitunut ja viittaa siihen , että myös hiivan SIRT2 ortologi Hst2p olisi myös spesifinen H4K16Ac:lle. Mutta H4K16Ac deasetylaatio SIRT2:n avulla ei kuitenkaan johda heterokromatiinin muodostukseen, vaan sen sijaan hyvin tärkeään tehtävään solusyklin kontrolloimisessa. ( Tämä on osoitettu hiiren alkion fibroblasteilla verrattaessa Sirt2-/- ja Sirt1-/- fibroblasteja mitoosissa: mitoottinen Sirt2-/- osoitti H4K16Ac hypoasetylaatiota, mutta tätä ei ilmentynyt Sirt1-/- fibroblasteissa). Mielenkiintoinen huomio oli, että H4K16Ac säätyy tiukasti solusyklin aikana. Sen huippupitoisuus on S-faasin aikana ja sen pitoisuus laskee hyvin vahvasti G2/M siirtymässä. SIRT2 esiintyy sytoplasmassa koko solusyklin aikana muulloin paitsi G2/M transitiossa, jolloin se sukkuloituu tuman puolelle deasetyloimaan kaiken H4K16Ac:n ennen mitoosiin (M) siirtymistä. .                                                                                                                                                       • Despite being localized chiefly in the cytoplasm, SIRT2 specifically deacetylates H4K16Ac and, to a much lesser extent, H3K9Ac. RNAi experiments show that loss of SIRT2 correlates to high levels of H4K16Ac, analogously to loss of SIRT1 (21). This activity has been conserved over evolution, as indicated by the fact that the SIRT2 yeast ortholog Hst2p is also highly specific for H4K16Ac. Unlike SIRT1, deacetylation of H4K16Ac by SIRT2 is not related to heterochromatin formation but instead has a very important role in cell cycle control, as evidenced by the fact that Sirt2−/− mouse embryonic fibroblasts (MEFs) exhibit H4K16Ac hypoacetylation during mitosis, whereas Sirt1−/− MEFs do not 21. Interestingly, H4K16Ac is tightly regulated during the cell cycle: its levels peak during S phase and drop dramatically in the G2/M transition. SIRT2 is present in the cytoplasm throughout the cell cycle except during the G2/M transition, when it is shuttled to the nucleus where it deacetylates H4K16Ac globally before entering mitosis (21, 29, 79                                                                                                 • Alunperin tulkittiin tämä globaali deasetylaatio mitoosiin siirtymisen edellytykseksi ottaen huomioon tämän histonitunnuksen relevanssi kromatiinin tiivistymisen estämisessä. Kuitenkin jatkotutkimukset osoittivat, että SIRT2:lla tapahtuva H4K16Ac:n deasetylaatio on varsinaisesti ylin säätö H4K20me1-kertymälle, monometyloidun histonin kertymän mahdollisuudelle.. Itseasiassa sitten ehdotettiin useita vuosia H4K16Ac -ja H4K20me1- merkkautuneitten histoneitten antagonismia, vastavaikutteisuutta. Tätä perusteltiin siten, että H4K16Ac omaa monometyloidun H4K20me1 metyylitransferaasin (HMT, PR-SET) aktiivisuuden estävää ominaisuutta. Kuitenkin tällainen oletettu antagonismi osoittautui ilmenevän vain G2/M:ssä ja taas muissa yhteyksissä H4K16Ac ja H4K20me1 näyttivät sijoittautuneen yhdessä samaan kohtaan . Siitä huolimatta tämän (G2/M vaiheen) antagonismin merkitsevyys piilee siinä relevantissa roolissa, mikä H4K20-mono-, di- tai trimetylaatiolla on solusyklin kontrolliin, kehitykseen, kromosomin tiivistymiseen, DNA:n korjaussignalointiin ja genomin stabiliteet tiin.            • This global deacetylation of H4K16Ac was originally interpreted as a prerequisite for mitotic entry, given the relevance of this mark in the inhibition of chromatin compaction. However, subsequent studies showed that deacetylation of H4K16Ac by SIRT2 during G2/M is actually paramount for regulating deposition of H4K20me1 31. In fact, an antagonism between H4K16Ac and H4K20me1 was proposed several years ago 32, based on the inhibitory effect that H4K16Ac has on the methyltransferase activity of the H4K20me1 HMT, PR‐SET7 (31, 32). However, this antagonism seems to occur only in G2/M; in other contexts, H4K16Ac and H4K20me1 have been shown to localize together 78. Nonetheless, the significance of this antagonism lies in the relevant role of H4K20 mono‐, di‐ or tri‐methylation in the control of cell cycle progression, development, chromosome compaction, DNA repair signaling and genome stability (7 9-83).                                                                           
 
 H4K20me1 , lysiiniinsä 20 monometyloitunut H4. H4K20me1 on esimerkiksi essentielli kromatiinin tiivistymisessä mitoosin aikana ja solusyklin progredioitumisen aikana. SIRT2 varsinaisesti säätelee H4K20me1- PR-SET7 histonimetyylitransferaasin aktiivisuutta eikä ainoastaan deasetyloimalla histonia H4K16Ac, vaan myös suoraan moduloimalla entsyymin PR SET7 aktiivisuutta ja dynamiikkaa. Saatujen tietojen mukaan tämä säätely on suoraan vaikuttamassa G2/M-tarkistuskohdan kontrollia. G2/M:n aikaisessa stressissä SIRT2 sitoutuu vahvasti (histonia metyloivaan) PR-SET/7-entsyymiin , mikä johtaa lisääntyneeseen H4K20me1:n määrään, ja tämä taas korreloi solusyklin blokeerautumiseen G2/M kohdassa stressin aikana. Lisäksi SIRT2 on hyvin tärkeä solusyklille ja nämä vaikutukset ulottuvat yli G2/M -transitiovaiheessa tapahtuvan H4K16- ja H4K20- histonien säätelyn. SIRT2 säätelee muita proteiineja myös muissa solusyklifaaseissa.                                                                                                   
   • For instance, H4K20me1 is essential for chromatin condensation during mitosis and cell cycle progression. As we discuss later, SIRT2 actually regulates the H4K20me1 activity of PR‐SET7, not only by deacetylating H4K16Ac but also by directly modulating the activity and dynamics of PR‐SET7. Data show that this regulation is directly involved in G2/M checkpoint control. Under stress during G2/M, SIRT2 binds strongly to PR‐SET7, leading to an increase in H4K20me1, which correlates to blocking of the cell cycle at G2/M 31. Moreover, SIRT2 is very important in the cell cycle and extends beyond regulation of H4K16 and H4K20 in G2/M: it also helps regulate important proteins in other phases (77), (84-86). 
 
 
.... 
 
 

SIRT2 controls the histone mark H4K20me1 during the cell cycle by regulating PR-SET7

Another major functional relationship between a histone deacetylase and a methyltransferases is that between SIRT2 and PR-SET7, for regulating cell cycle progression. As we mentioned earlier, SIRT2 is crucial for regulating H4K16Ac throughout the cell cycle and for establishing PR-SET7-mediated H4K20me1 during early mitosis. H4K20me1 is established by PR-SET7 in late G2/early M and is critical for metaphasic chromosome compaction during mitosis and mitotic exit [83, 118] as well as in DNA repair and replication [119-121]. During late M/early G1, H4K20me1 is subsequently methylated into H4K20me2 (by SUV420H1) or H4K20me3 (by SUV420H2), which are required for DNA repair or for heterochromatin structure formation, respectively [79-81].

Evidence suggests that during mitosis SIRT2 regulates H4K20me1 deposition via PR-SET7** and promotes the spread of H4K20me1. The proposed model involves several steps, beginning with the arrival of PR-SET7 to specific chromatin regions during late G2, where it recruits SIRT2 during G2/M. In turn, SIRT2 promotes the enzymatic activity of PR-SET7 through its deacetylation at K90 and the deacetylation of H4K16Ac from the neighboring nucleosome. Deacetylation of PR-SET7 induces its mobilization and SIRT2-bound PR-SET7 monomethylates H4K20 in the adjacent nucleosome. This occurs successively and enables the spread of PR-SET7 binding to chromatin as well as subsequent H4K20me1 deposition [31] (Fig. 2). Interestingly, a very recent paper suggests that PR-SET7 might in turn control H4K16Ac (as well as H4K20me3) to regulate the pausing dynamics of RNA polymerase II (Pol II) [122].

Interestingly, under stress during G2/M, the interaction between SIRT2 and PR-SET7 increases significantly, as do global H4K20me1 levels, suggesting a previously unknown G2/M checkpoint mechanism. This would be the first link between H4K20me1 and a cell cycle checkpoint, and between H4K20me1 and SIRT2-dependent stress response. These findings corroborate a dynamic role for sirtuins in controlling the cell cycle through modulation of epigenetic regulatory information.

 

 

Lisäys: Genecards_** PR-SET7 https://www.genecards.org/cgi-bin/carddisp.pl?gene=KMT5A&keywords=PR-SET7 

  • GeneCards Symbol: KMT5A 2
  • Lysine Methyltransferase 5A 2 3 5
  • PR-Set7 2 3 4 5
  • SET07 2 3 4 5
  • SET8 2 3 4 5
  • SETD8 3 4 5
  • SET Domain Containing (Lysine Methyltransferase) 8 2 3
  • Lysine (K)-Specific Methyltransferase 5A 2 3
  • Histone-Lysine N-Methyltransferase KMT5A 3 4
  • PR/SET Domain-Containing Protein 07 3 4
  • N-Lysine Methyltransferase KMT5A 3 4
  • SET Domain-Containing Protein 8 3 4
  • Lysine N-Methyltransferase 5A 3 4

Post-translational modifications for KMT5A Gene

  • Acetylated at Lys-162; does not affect methyltransferase activity.
    Deacetylated at Lys-162 possibly by SIRT2; does not change methyltransferase activity.
    ( Q9NQR1-KMT5A_HUMAN )
  • Ubiquitinated and degraded by the DCX(DTL) complex. ( Q9NQR1-KMT5A_HUMAN )
  • Ubiquitination at Lys236 and Lys275 ( NX_Q9NQR1 [NX_Q9NQR1-1] )
  • Modification sites at PhosphoSitePlus ( Q9NQR1 )
  • Glycosylation from GlyGen (Q9NQR1) 1 site, 1 O-linked glycan (1 site)  

Protein-lysine N-methyltransferase that monomethylates both histones and non-histone proteins (PubMed:12086618,
Specifically monomethylates 'Lys-20' of histone H4 (H4K20me1) (PubMed:12086618, 12121615,
H4K20me1 is enriched during mitosis and represents a specific tag for epigenetic transcriptional repression (PubMed:12086618,
Mainly functions in euchromatin regions, thereby playing a central role in the silencing of euchromatic genes (PubMed:12086618
Required for cell proliferation, probably by contributing to the maintenance of proper higher-order structure of DNA during mitosis (PubMed:12086618,
Involved in chromosome condensation and proper cytokinesis (PubMed:12086618, 12121615,
Nucleosomes are preferred as substrate compared to free histones (PubMed:12086618, 12121615,
Mediates monomethylation of p53/TP53 at 'Lys-382', leading to repress p53/TP53-target genes (PubMed:17707234).
Plays a negative role in TGF-beta response regulation and a positive role in  

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