Literature DB >> 28228643

A chemical probe toolbox for dissecting the cancer epigenome.

Jake Shortt1,2,3, Christopher J Ott4,5,6, Ricky W Johnstone1,2, James E Bradner4,5,6.   

Abstract

Cancer cell hallmarks are underpinned by transcriptional programmes operating in the context of a dynamic and complicit epigenomic environment. Somatic alterations of chromatin modifiers are among the most prevalent cancer perturbations. There is a pressing need for targeted chemical probes to dissect these complex, interconnected gene regulatory circuits. Validated chemical probes empower mechanistic research while providing the pharmacological proof of concept that is required to translate drug-like derivatives into therapy for cancer patients. In this Review, we describe chemical probe development for epigenomic effector proteins that are linked to cancer pathogenesis. By annotating these reagents, we aim to share our perspectives on an informative 'epigenomic toolbox' of broad utility to the research community.

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Year:  2017        PMID： 28228643     DOI： 10.1038/nrc.2016.148

Source DB:  PubMed          Journal:  Nat Rev Cancer        ISSN： 1474-175X            Impact factor:   60.716


  286 in total

Review 1.  Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders.

Authors:  Katrina J Falkenberg; Ricky W Johnstone
Journal:  Nat Rev Drug Discov       Date:  2014-08-18       Impact factor: 84.694

2.  Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells.

Authors:  M Göttlicher; S Minucci; P Zhu; O H Krämer; A Schimpf; S Giavara; J P Sleeman; F Lo Coco; C Nervi; P G Pelicci; T Heinzel
Journal:  EMBO J       Date:  2001-12-17       Impact factor: 11.598

3.  Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan.

Authors:  Konrad T Howitz; Kevin J Bitterman; Haim Y Cohen; Dudley W Lamming; Siva Lavu; Jason G Wood; Robert E Zipkin; Phuong Chung; Anne Kisielewski; Li-Li Zhang; Brandy Scherer; David A Sinclair
Journal:  Nature       Date:  2003-08-24       Impact factor: 49.962

4.  EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation.

Authors:  Wendy Béguelin; Relja Popovic; Matt Teater; Yanwen Jiang; Karen L Bunting; Monica Rosen; Hao Shen; Shao Ning Yang; Ling Wang; Teresa Ezponda; Eva Martinez-Garcia; Haikuo Zhang; Yupeng Zheng; Sharad K Verma; Michael T McCabe; Heidi M Ott; Glenn S Van Aller; Ryan G Kruger; Yan Liu; Charles F McHugh; David W Scott; Young Rock Chung; Neil Kelleher; Rita Shaknovich; Caretha L Creasy; Randy D Gascoyne; Kwok-Kin Wong; Leandro Cerchietti; Ross L Levine; Omar Abdel-Wahab; Jonathan D Licht; Olivier Elemento; Ari M Melnick
Journal:  Cancer Cell       Date:  2013-05-13       Impact factor: 31.743

Review 5.  The histone LSD1 demethylase in stemness and cancer transcription programs.

Authors:  Stefano Amente; Luigi Lania; Barbara Majello
Journal:  Biochim Biophys Acta       Date:  2013-05-16

Review 6.  Sorting out functions of sirtuins in cancer.

Authors:  M Roth; W Y Chen
Journal:  Oncogene       Date:  2013-04-22       Impact factor: 9.867

7.  Impaired DNA damage response, genome instability, and tumorigenesis in SIRT1 mutant mice.

Authors:  Rui-Hong Wang; Kundan Sengupta; Cuiling Li; Hyun-Seok Kim; Liu Cao; Cuiying Xiao; Sangsoo Kim; Xiaoling Xu; Yin Zheng; Beverly Chilton; Rong Jia; Zhi-Ming Zheng; Ettore Appella; Xin Wei Wang; Thomas Ried; Chu-Xia Deng
Journal:  Cancer Cell       Date:  2008-10-07       Impact factor: 31.743

8.  Proteomic and bioinformatic analysis of mammalian SWI/SNF complexes identifies extensive roles in human malignancy.

Authors:  Cigall Kadoch; Diana C Hargreaves; Courtney Hodges; Laura Elias; Lena Ho; Jeff Ranish; Gerald R Crabtree
Journal:  Nat Genet       Date:  2013-05-05       Impact factor: 38.330

9.  Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

Authors:  Mark A Dawson; Rab K Prinjha; Antje Dittmann; George Giotopoulos; Marcus Bantscheff; Wai-In Chan; Samuel C Robson; Chun-wa Chung; Carsten Hopf; Mikhail M Savitski; Carola Huthmacher; Emma Gudgin; Dave Lugo; Soren Beinke; Trevor D Chapman; Emma J Roberts; Peter E Soden; Kurt R Auger; Olivier Mirguet; Konstanze Doehner; Ruud Delwel; Alan K Burnett; Phillip Jeffrey; Gerard Drewes; Kevin Lee; Brian J P Huntly; Tony Kouzarides
Journal:  Nature       Date:  2011-10-02       Impact factor: 49.962

10.  A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

Authors:  Laurens Kruidenier; Chun-wa Chung; Zhongjun Cheng; John Liddle; KaHing Che; Gerard Joberty; Marcus Bantscheff; Chas Bountra; Angela Bridges; Hawa Diallo; Dirk Eberhard; Sue Hutchinson; Emma Jones; Roy Katso; Melanie Leveridge; Palwinder K Mander; Julie Mosley; Cesar Ramirez-Molina; Paul Rowland; Christopher J Schofield; Robert J Sheppard; Julia E Smith; Catherine Swales; Robert Tanner; Pamela Thomas; Anthony Tumber; Gerard Drewes; Udo Oppermann; Dinshaw J Patel; Kevin Lee; David M Wilson
Journal:  Nature       Date:  2012-08-16       Impact factor: 49.962
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  35 in total

1.  Eradication of Central Nervous System Leukemia of T-Cell Origin with a Brain-Permeable LSD1 Inhibitor.

Authors:  Shiori Saito; Jiro Kikuchi; Daisuke Koyama; Shin Sato; Hiroo Koyama; Naoki Osada; Yoshiaki Kuroda; Koshi Akahane; Takeshi Inukai; Takashi Umehara; Yusuke Furukawa
Journal:  Clin Cancer Res       Date:  2018-12-05       Impact factor: 12.531

2.  Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7.

Authors:  Kelsey N Lamb; Daniel Bsteh; Sarah N Dishman; Hagar F Moussa; Huitao Fan; Jacob I Stuckey; Jacqueline L Norris; Stephanie H Cholensky; Dongxu Li; Jingkui Wang; Cari Sagum; Benjamin Z Stanton; Mark T Bedford; Kenneth H Pearce; Terry P Kenakin; Dmitri B Kireev; Gang Greg Wang; Lindsey I James; Oliver Bell; Stephen V Frye
Journal:  Cell Chem Biol       Date:  2019-08-15       Impact factor: 8.116

3.  A chemical probe toolbox for dissecting the cancer epigenome.

Authors:  Jake Shortt; Christopher J Ott; Ricky W Johnstone; James E Bradner
Journal:  Nat Rev Cancer       Date:  2017-03-23       Impact factor: 60.716

4.  Opportunities for targeting gene regulatory factors in B-cell acute lymphoblastic leukemia.

Authors:  Christopher J Ott
Journal:  Int J Hematol Oncol       Date:  2017-11-20

Review 5.  Inhibitors and chemical probes for molecular chaperone networks.

Authors:  Jason E Gestwicki; Hao Shao
Journal:  J Biol Chem       Date:  2018-09-13       Impact factor: 5.157

6.  Loss of Methylation Modification Marks the Presence of Psoriasis.

Authors:  Brian C Capell; John T Seykora
Journal:  J Invest Dermatol       Date:  2020-06       Impact factor: 8.551

Review 7.  Reactivation of endogenous retroviral elements via treatment with DNMT- and HDAC-inhibitors.

Authors:  Michael Daskalakis; David Brocks; Yi-Hua Sheng; Md Saiful Islam; Alzbeta Ressnerova; Yassen Assenov; Till Milde; Ina Oehme; Olaf Witt; Ashish Goyal; Alexander Kühn; Mark Hartmann; Dieter Weichenhan; Manfred Jung; Christoph Plass
Journal:  Cell Cycle       Date:  2018-04-30       Impact factor: 4.534

8.  Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.

Authors:  Shuai Liu; Hailemichael O Yosief; Lingling Dai; He Huang; Gagan Dhawan; Xiaofeng Zhang; Alex M Muthengi; Justin Roberts; Dennis L Buckley; Jennifer A Perry; Lei Wu; James E Bradner; Jun Qi; Wei Zhang
Journal:  J Med Chem       Date:  2018-08-30       Impact factor: 7.446

Review 9.  Targeting the epigenetic regulation of antitumour immunity.

Authors:  Simon J Hogg; Paul A Beavis; Mark A Dawson; Ricky W Johnstone
Journal:  Nat Rev Drug Discov       Date:  2020-09-14       Impact factor: 84.694

Review 10.  The Chemical Biology of Reversible Lysine Post-translational Modifications.

Authors:  Zhipeng A Wang; Philip A Cole
Journal:  Cell Chem Biol       Date:  2020-07-21       Impact factor: 8.116
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