The emerging role of lysine methyltransferase SETD8 in human diseases

被引：71

作者：

Milite, Ciro ^{[1
,2
]}

Feoli, Alessandra ^{[1
,2
,3
]}

Viviano, Monica ^{[1
,2
]}

Rescigno, Donatella ^{[1
,2
,3
]}

Cianciulli, Agostino ^{[1
,2
,3
]}

Balzano, Amodio Luca ^{[1
,2
,3
]}

Mai, Antonello ^{[4
]}

Castellano, Sabrina ^{[1
,2
,5
]}

Sbardella, Gianluca ^{[1
,2
]}

机构：

[1] Univ Salerno, Dipartimento Farm, Via Giovanni Paolo 2 132, I-84084 Salerno, Italy

[2] Univ Salerno, Epigenet Med Chem Lab, Via Giovanni Paolo 2 132, I-84084 Salerno, Italy

[3] Univ Salerno, Programma Dottorato Ric Sci Farmaco, Via Giovanni Paolo 2 132, I-84084 Salerno, Italy

[4] Sapienza Univ Roma, Dipartimento Chim & Tecnol Farmaco, Ist Pasteur, Fdn Cenci Bolognetti, Ple A Moro 5, I-00185 Rome, Italy

[5] Univ Salerno, Dipartimento Med & Chirurg, Via Salvador Allende, I-84081 Salerno, Italy

来源：

CLINICAL EPIGENETICS | 2016年 / 8卷

关键词：

SMALL-MOLECULE INHIBITORS; 3' UNTRANSLATED REGION; MIR-502; BINDING-SITE; HISTONE H4-LYSINE 20; ACIDS B-E; CELL-CYCLE; PROTEIN METHYLTRANSFERASES; COMPETITIVE INHIBITOR; MIR-502-BINDING SITE; MARINE SEDIMENT;

D O I：

10.1186/s13148-016-0268-4

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

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.

引用

页数：15

共 34 条

[31] SET8 plays a role in controlling G1/S transition by blocking lysine acetylation in histone through binding to H4N-terminal tail
Yin, Yinliang
Yu, Vivian C.
Zhu, Guang
Chang, Donald C.
CELL CYCLE, 2008, 7 (10) : 1423 - 1432
[32] Role of ORF74-Encoded Viral G Protein-Coupled Receptor in Human Herpesvirus 8 Lytic Replication
Sandford, Gordon
Choi, Young Bong
Nicholas, John
JOURNAL OF VIROLOGY, 2009, 83 (24) : 13009 - 13014
[33] Histone methyltransferase SET8 is regulated by miR-192/215 and induces oncogene-induced senescence via p53-dependent DNA damage in human gastric carcinoma cells
Zhang, Xiaojing
Peng, Yin
Yuan, Yuan
Gao, Yuli
Hu, Fan
Wang, Jian
Zhu, Xiaohui
Feng, Xianling
Cheng, Yulan
Wei, Yanjie
Fan, Xinmin
Xie, Yaohong
Lv, Yansi
Ashktorab, Hassan
Smoot, Duane
Li, Song
Meltzer, Stephen J.
Hou, Gangqiang
Jin, Zhe
CELL DEATH & DISEASE, 2020, 11 (10)
[34] Glucuronidation of piceatannol by human liver microsomes: major role of UGT1A1, UGT1A8 and UGT1A10
Miksits, Michaela
Maier-Salamon, Alexandra
Thanh Phuong Nha Vo
Sulyok, Michael
Schuhmacher, Rainer
Szekeres, Thomas
Jaeger, Walter
JOURNAL OF PHARMACY AND PHARMACOLOGY, 2010, 62 (01) : 47 - 54

← 1 2 3 4 →