The emerging role of lysine methyltransferase SETD8 in human diseases

被引：70
|
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.
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页数：15
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