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.
引用
收藏
页数：15
相关论文
共 50 条
  • [21] Histone Methyltransferase Setd8 Represses Gata2 Expression and Regulates Erythroid Maturation
    Malik, Jeffrey
    Getman, Michael
    Steiner, Laurie A.
    MOLECULAR AND CELLULAR BIOLOGY, 2015, 35 (12) : 2059 - 2072
  • [22] The histone methyltransferase Setd8 acts in concert with c-Myc and is required to maintain skin
    Driskell, Iwona
    Oda, Hisanobu
    Blanco, Sandra
    Nascimento, Elisabete
    Humphreys, Peter
    Frye, Michaela
    EMBO JOURNAL, 2012, 31 (03): : 616 - 629
  • [23] A Dual Role for the Histone Methyltransferase PR-SET7/SETD8 and Histone H4 Lysine 20 Monomethylation in the Local Regulation of RNA Polymerase II Pausing
    Kapoor-Vazirani, Priya
    Vertino, Paula M.
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2014, 289 (11) : 7425 - 7437
  • [24] Discovery of selective inhibitors for lysine methyltransferases EZH2/EZH1 and SETD8
    Ma, Anqi
    Xu, Bowen
    Doan On
    Yu, Wenyu
    Konze, Kyle
    Butler, Kyle
    Li, Fengling
    Vedadi, Masoud
    Brown, Peter
    Wang, Gang
    Jin, Jian
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2015, 250
  • [25] The Role and Mechanism of Lysine Methyltransferase and Arginine Methyltransferase in Kidney Diseases
    Zhou, Xun
    Chen, Hui
    Li, Jinqing
    Shi, Yingfeng
    Zhuang, Shougang
    Liu, Na
    FRONTIERS IN PHARMACOLOGY, 2022, 13
  • [26] Oligomerization and Auto-methylation of the Human Lysine Methyltransferase SETD6
    Weil, Lital Estrella
    Shmidov, Yulia
    Kublanovsky, Margarita
    Morgenstern, David
    Feldman, Michal
    Bitton, Ronit
    Levy, Dan
    JOURNAL OF MOLECULAR BIOLOGY, 2018, 430 (21) : 4359 - 4368
  • [27] Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth
    Rosa Della Monica
    Michela Buonaiuto
    Mariella Cuomo
    Cristina Pagano
    Federica Trio
    Davide Costabile
    Giulia de Riso
    Francesca Sveva Cicala
    Maddalena Raia
    Raduan Ahmed Franca
    Marialaura Del Basso De Caro
    Domenico Sorrentino
    Giovanna Navarra
    Laura Coppola
    Lorella Tripodi
    Lucio Pastore
    Juergen Hench
    Stephan Frank
    Claudio Schonauer
    Giuseppe Catapano
    Maurizio Bifulco
    Lorenzo Chiariotti
    Roberta Visconti
    Cell Death & Disease, 14
  • [28] Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth
    Della Monica, Rosa
    Buonaiuto, Michela
    Cuomo, Mariella
    Pagano, Cristina
    Trio, Federica
    Costabile, Davide
    de Riso, Giulia
    Cicala, Francesca Sveva
    Raia, Maddalena
    Franca, Raduan Ahmed
    Del Basso De Caro, Marialaura
    Sorrentino, Domenico
    Navarra, Giovanna
    Coppola, Laura
    Tripodi, Lorella
    Pastore, Lucio
    Hench, Juergen
    Frank, Stephan
    Schonauer, Claudio
    Catapano, Giuseppe
    Bifulco, Maurizio
    Chiariotti, Lorenzo
    Visconti, Roberta
    CELL DEATH & DISEASE, 2023, 14 (09)
  • [29] Dual role of the histone methyltransferase PR-SET7/SETD8 in the local regulation of Pol II promoter-proximal pausing
    Kapoor, Priya
    Vertino, Paula M.
    CANCER RESEARCH, 2013, 73
  • [30] The Histone Methyltransferase Setd8 Alters the Chromatin Landscape and Regulates the Expression of Key Transcription Factors during Erythroid Differentiation
    Lillis, Jacquelyn
    Malik, Jeffrey
    Couch, Tyler A.
    Getman, Michael
    Steiner, Laurie A.
    BLOOD, 2018, 132
12345