Pharmacological targeting of the cancer epigenome

被引：25

作者：

Mabe, Nathaniel W. ^{[1
,2
]}

Perry, Jennifer A. ^{[1
]}

Malone, Clare F. ^{[1
,2
]}

Stegmaier, Kimberly ^{[1
,2
,3
]}

机构：

[1] Dana Farber Canc Inst, Dept Pediat Oncol, Boston, MA 02215 USA

[2] Broad Inst & Harvard, Cambridge, MA 02142 USA

[3] Boston Childrens Hosp, Div Hematol Oncol, Boston, MA 02115 USA

来源：

NATURE CANCER | 2024年 / 5卷 / 06期

基金：

美国国家卫生研究院;

关键词：

METHYLTRANSFERASE GENE EZH2; CELL LUNG-CANCER; SELECTIVE-INHIBITION; HISTONE ACETYLATION; SYNTHETIC LETHALITY; LYSINE ACETYLATION; CRYSTAL-STRUCTURE; YEATS DOMAIN; OPEN-LABEL; POLYCOMB;

D O I：

10.1038/s43018-024-00777-2

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including disease initiation, maintenance and therapy resistance. As a result, there have been advances in the development and evaluation of epigenetic therapies for cancer, revealing substantial promise but also challenges. Three epigenetic inhibitor classes are approved in the USA, and many more are currently undergoing clinical investigation. In this Review, we discuss recent developments for each epigenetic drug class and their implications for therapy, as well as highlight new insights into the role of epigenetics in cancer. Stegmaier and colleagues provide a review on the latest development in targeting the cancer epigenome, give an overview of distinct drug classes, and discuss therapeutic possibilities and challenges.

引用

页码：844 / 865

页数：22

共 230 条

[1] Histone H3K36me2-Specific Methyltransferase ASH1L Promotes MLL-AF9-Induced Leukemogenesis [J].

Aljazi, Mohammad B. ;

Gao, Yuen ;

Wu, Yan ;

Mias, George, I ;

He, Jin .

FRONTIERS IN ONCOLOGY, 2021, 11

[2] The molecular hallmarks of epigenetic control [J].

Allis, C. David ;

Jenuwein, Thomas .

NATURE REVIEWS GENETICS, 2016, 17 (08) :487-500

[3] Mex3a marks drug-tolerant persister colorectal cancer cells that mediate relapse after chemotherapy [J].

Alvarez-Varela, Adrian ;

Novellasdemunt, Laura ;

Barriga, Francisco M. ;

Hernando-Momblona, Xavier ;

Canellas-Socias, Adria ;

Cano-Crespo, Sara ;

Sevillano, Marta ;

Cortina, Carme ;

Stork, Diana ;

Morral, Clara ;

Turon, Gemma ;

Slebe, Felipe ;

Jimenez-Gracia, Laura ;

Caratu, Ginevra ;

Jung, Peter ;

Stassi, Giorgio ;

Heyn, Holger ;

Tauriello, Daniele V. F. ;

Mateo, Lidia ;

Tejpar, Sabine ;

Sancho, Elena ;

Stephan-Otto Attolini, Camille ;

Batlle, Eduard .

NATURE CANCER, 2022, 3 (09) :1052-+

[4] EMT: 2016 [J].

Angela Nieto, M. ;

Huang, Ruby Yun-Ju ;

Jackson, Rebecca A. ;

Thiery, Jean Paul .

CELL, 2016, 166 (01) :21-45

[5] EWS::FLI1 and HOXD13 Control Tumor Cell Plasticity in Ewing Sarcoma [J].

Apfelbaum, April A. ;

Wu, Feinan ;

Hawkins, Allegra G. ;

Magnuson, Brian ;

Jime, Jennifer A. ;

Taylor, Sean D. ;

Wrenn, Emma D. ;

Waltner, Olivia ;

Pfaltzgraff, Elise R. ;

Song, Jane Y. ;

Hall, Cody ;

Wellik, Deneen M. ;

Ljungman, Mats ;

Furlan, Scott N. ;

Ryan, Russell J. H. ;

Sarthy, Jay F. ;

Lawlor, Elizabeth R. .

CLINICAL CANCER RESEARCH, 2022, 28 (20) :4466-4478

[6] Cell-Based Ligand Discovery for the ENL YEATS Domain [J].

Asiaban, Joshua N. ;

Milosevich, Natalia ;

Chen, Emily ;

Bishop, Timothy R. ;

Wang, Justin ;

Zhang, Yuxiang ;

Ackerman, Christopher J. ;

Hampton, Eric N. ;

Young, Travis S. ;

Hull, Mitchell V. ;

Cravatt, Benjamin F. ;

Erb, Michael A. .

ACS CHEMICAL BIOLOGY, 2020, 15 (04) :895-903

[7] BCOR involvement in cancer [J].

Astolfi, Annalisa ;

Fiore, Michele ;

Melchionda, Fraia ;

Indio, Valentina ;

Bertuccio, Salvatore N. ;

Pession, Andrea .

EPIGENOMICS, 2019, 11 (07) :835-855

[8] Targeting NOTCH activation in small cell lung cancer through LSD1 inhibition [J].

Augert, Arnaud ;

Eastwood, Emily ;

Ibrahim, Ali H. ;

Wu, Nan ;

Grunblatt, Eli ;

Basom, Ryan ;

Liggitt, Denny ;

Eaton, Keith D. ;

Martins, Renato ;

Poirier, John T. ;

Rudin, Charles M. ;

Milletti, Francesca ;

Cheng, Wei-Yi ;

Mack, Fiona ;

MacPherson, David .

SCIENCE SIGNALING, 2019, 12 (567)

[9] Loss of G9a preserves mutation patterns but increases chromatin accessibility, genomic instability and aggressiveness in skin tumours [J].

Avgustinova, Alexandra ;

Symeonidi, Aikaterini ;

Castellanos, Andres ;

Urdiroz-Urricelqui, Uxue ;

Sole-Boldo, Llorenc ;

Martin, Merce ;

Perez-Rodriguez, Ivan ;

Prats, Neus ;

Lehner, Ben ;

Supek, Fran ;

Aznar Benitah, Salvador .

NATURE CELL BIOLOGY, 2018, 20 (12) :1400-+

[10] Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth [J].

Baell, Jonathan B. ;

Leaver, David J. ;

Hermans, Stefan J. ;

Kelly, Gemma L. ;

Brennan, Margs S. ;

Downer, Natalie L. ;

Nguyen, Nghi ;

Wichmann, Johannes ;

Mcrae, Helen M. ;

Yang, Yuqing ;

Cleary, Ben ;

Lagiakos, H. Rachel ;

Mieruszynski, Stephen ;

Pacini, Guido ;

Vanyai, Hannah K. ;

Bergamasco, Maria I. ;

May, Rose E. ;

Davey, Bethany K. ;

Morgan, Kimberly J. ;

Sealey, Andrew J. ;

Wang, Beinan ;

Zamudio, Natasha ;

Wilcox, Stephen ;

Garnham, Alexandra L. ;

Sheikh, Bilal N. ;

Aubrey, Brandon J. ;

Doggett, Karen ;

Chung, Matthew C. ;

de Silva, Melanie ;

Bentley, John ;

Pilling, Pat ;

Hattarki, Meghan ;

Dolezal, Olan ;

Dennis, Matthew L. ;

Falk, Hendrik ;

Ren, Bin ;

Charman, Susan A. ;

White, Karen L. ;

Rautela, Jai ;

Newbold, Andrea ;

Hawkins, Edwin D. ;

Johnstone, Ricky W. ;

Huntington, Nicholas D. ;

Peat, Thomas S. ;

Heath, Joan K. ;

Strasser, Andreas ;

Parker, Michael W. ;

Smyth, Gordon K. ;

Street, Ian P. ;

Monahan, Brendon J. .

NATURE, 2018, 560 (7717) :253-+

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