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Epigenetics Collection

There are a number of important components that affect epigenetic processes. Some compounds that inhibit the actions of key enzymes involved in epigenetic processes have been approved by the FDA, demonstrating that interference in these processes can result in therapeutically beneficial outcomes. In addition, so-called epigenetic "reader" domains have emerged as targets with therapeutic potential. However, some challenges still need to be overcome for this field to progress.

ACS Chemical Biology, ACS Medicinal Chemistry Letters, Biochemistry, and Journal of Medicinal Chemistry have created a collection of articles that showcase some of the most significant recent research in the epigenetics area. We hope this collection will further stimulate interdisciplinary research in epigenetics.

In addition to this collection of previously published research, ACS Chemical Biology, ACS Medicinal Chemistry Letters, Biochemistry, and Journal of Medicinal Chemistry published Special Issues on "Epigenetics"

Click on the covers to view each special issue.

Go to Journal of Medicinal Chemistry
Go to ACS Medicinal Chemistry Letters
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Articles

Article figure
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
  • Emmanuel H. Demont
  • , 
  • Paul Bamborough*
  • , 
  • Chun-wa Chung
  • , 
  • Peter D. Craggs
  • , 
  • David Fallon
  • , 
  • Laurie J. Gordon
  • , 
  • Paola Grandi
  • , 
  • Clare I. Hobbs
  • , 
  • Jameed Hussain
  • , 
  • Emma J. Jones
  • , 
  • Armelle Le Gall
  • , 
  • Anne-Marie Michon
  • , 
  • Darren J. Mitchell
  • , 
  • Rab K. Prinjha
  • , 
  • Andy D. Roberts
  • , 
  • Robert J. Sheppard
  • , and 
  • Robert J. Watson
ACS Med. Chem. Lett. 2014, 5, 11, 1190-1195
  • Open Access
  • Editors Choice
Publication Date (Web):September 10, 2014
Article figure
Chemical Probes of Histone Lysine Methyltransferases
  • H. Ümit Kaniskan
  •  and 
  • Jian Jin*
ACS Chem. Biol. 2015, 10, 1, 40-50
  • Open Access
Publication Date (Web):November 25, 2014
Article figure
Chromodomain Antagonists That Target the Polycomb-Group Methyllysine Reader Protein Chromobox Homolog 7 (CBX7)
  • Chakravarthi Simhadri
  • , 
  • Kevin D. Daze
  • , 
  • Sarah F. Douglas
  • , 
  • Taylor T. H. Quon
  • , 
  • Amarjot Dev
  • , 
  • Michael C. Gignac
  • , 
  • Fangni Peng
  • , 
  • Markus Heller
  • , 
  • Martin J. Boulanger
  • , 
  • Jeremy E. Wulff
  • , and 
  • Fraser Hof*
J. Med. Chem. 2014, 57, 7, 2874-2883
    Publication Date (Web):March 13, 2014
    Article figure
    Synthesis and Evaluation of Novel Cyclic Peptide Inhibitors of Lysine-Specific Demethylase 1
    • Isuru R. Kumarasinghe
    •  and 
    • Patrick M. Woster*
    ACS Med. Chem. Lett. 2014, 5, 1, 29-33
    • Open Access
    Publication Date (Web):November 8, 2013
    Article figure
    Metabolic Mechanisms of Epigenetic Regulation
    • Jordan L. Meier
    ACS Chem. Biol. 2013, 8, 12, 2607-2621
      Publication Date (Web):November 14, 2013
      Article figure
      High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction
      • Shihan He
      • , 
      • Timothy J. Senter
      • , 
      • Jonathan Pollock
      • , 
      • Changho Han
      • , 
      • Sunil Kumar Upadhyay
      • , 
      • Trupta Purohit
      • , 
      • Rocco D. Gogliotti
      • , 
      • Craig W. Lindsley
      • , 
      • Tomasz Cierpicki
      • , 
      • Shaun R. Stauffer
      • , and 
      • Jolanta Grembecka*
      J. Med. Chem. 2014, 57, 4, 1543-1556
      • Open Access
      Publication Date (Web):January 28, 2014
      Article figure
      Binding Hotspots of BAZ2B Bromodomain: Histone Interaction Revealed by Solution NMR Driven Docking
      • Fleur M. Ferguson
      • , 
      • David M. Dias
      • , 
      • João P. G. L. M. Rodrigues
      • , 
      • Hans Wienk
      • , 
      • Rolf Boelens
      • , 
      • Alexandre M. J. J. Bonvin
      • , 
      • Chris Abell
      • , and 
      • Alessio Ciulli*
      Biochemistry 2014, 53, 42, 6706-6716
      • Open Access
      Publication Date (Web):September 30, 2014
      Article figure
      Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
      • Olivier Mirguet*
      • , 
      • Romain Gosmini
      • , 
      • Jérôme Toum
      • , 
      • Catherine A. Clément
      • , 
      • Mélanie Barnathan
      • , 
      • Jean-Marie Brusq
      • , 
      • Jacqueline E. Mordaunt
      • , 
      • Richard M. Grimes
      • , 
      • Miriam Crowe
      • , 
      • Olivier Pineau
      • , 
      • Myriam Ajakane
      • , 
      • Alain Daugan
      • , 
      • Phillip Jeffrey
      • , 
      • Leanne Cutler
      • , 
      • Andrea C. Haynes
      • , 
      • Nicholas N. Smithers
      • , 
      • Chun-wa Chung
      • , 
      • Paul Bamborough
      • , 
      • Iain J. Uings
      • , 
      • Antonia Lewis
      • , 
      • Jason Witherington
      • , 
      • Nigel Parr*
      • , 
      • Rab K. Prinjha
      • , and 
      • Edwige Nicodème
      J. Med. Chem. 2013, 56, 19, 7501-7515
        Publication Date (Web):September 9, 2013
        Article figure
        Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2
        • Kanchan Devkota
        • , 
        • Brian Lohse
        • , 
        • Qing Liu
        • , 
        • Ming-Wei Wang
        • , 
        • Dan Stærk
        • , 
        • Jens Berthelsen*
        • , and 
        • Rasmus Prætorius Clausen*
        ACS Med. Chem. Lett. 2014, 5, 4, 293-297
          Publication Date (Web):January 31, 2014
          Article figure
          Structural Investigations of the Nickel-Induced Inhibition of Truncated Constructs of the JMJD2 Family of Histone Demethylases Using X-ray Absorption Spectroscopy
          • Nitai Charan Giri
          • , 
          • Lisa Passantino
          • , 
          • Hong Sun
          • , 
          • Maria Antonietta Zoroddu
          • , 
          • Max Costa
          • , and 
          • Michael J. Maroney*
          Biochemistry 2013, 52, 24, 4168-4183
            Publication Date (Web):May 21, 2013
            Article figure
            A Chemical Strategy for the Cell-Based Detection of HDAC Activity
            • Himashinie V. K. Diyabalanage
            • , 
            • Genevieve C. Van de Bittner
            • , 
            • Emily L. Ricq
            • , and 
            • Jacob M. Hooker*
            ACS Chem. Biol. 2014, 9, 6, 1257-1262
            • Open Access
            Publication Date (Web):April 28, 2014
            Article figure
            The Role of Enhancer of Zeste Homologue 2 Inhibitors in Controlling Epigenetics and Their Potential for Cancer Treatment
            • Ahmed F. Abdel-Magid*
            ACS Med. Chem. Lett. 2015, 6, 2, 108-109
            • Free to Read Access
            Publication Date (Web):January 8, 2015
            Article figure
            DNA Cytosine Methylation: Structural and Thermodynamic Characterization of the Epigenetic Marking Mechanism
            • Jin Yang
            • , 
            • Lee Lior-Hoffmann
            • , 
            • Shenglong Wang
            • , 
            • Yingkai Zhang*
            • , and 
            • Suse Broyde*
            Biochemistry 2013, 52, 16, 2828-2838
              Publication Date (Web):March 26, 2013
              Article figure
              Identification of Novel Inhibitors of DNA Methylation by Screening of a Chemical Library
              • Alexandre Ceccaldi
              • , 
              • Arumugam Rajavelu
              • , 
              • Sergey Ragozin
              • , 
              • Catherine Sénamaud-Beaufort
              • , 
              • Pavel Bashtrykov
              • , 
              • Noé Testa
              • , 
              • Hana Dali-Ali
              • , 
              • Christine Maulay-Bailly
              • , 
              • Séverine Amand
              • , 
              • Dominique Guianvarc’h
              • , 
              • Albert Jeltsch*
              • , and 
              • Paola B. Arimondo*
              ACS Chem. Biol. 2013, 8, 3, 543-548
                Publication Date (Web):January 8, 2013
                Article figure
                Unusual Characteristics of the DNA Binding Domain of Epigenetic Regulatory Protein MeCP2 Determine Its Binding Specificity
                • Sergei Khrapunov
                • , 
                • Christopher Warren
                • , 
                • Huiyong Cheng
                • , 
                • Esther R. Berko
                • , 
                • John M. Greally
                • , and 
                • Michael Brenowitz*
                Biochemistry 2014, 53, 21, 3379-3391
                • Open Access
                Publication Date (Web):May 14, 2014
                Article figure
                Degron Protease Blockade Sensor to Image Epigenetic Histone Protein Methylation in Cells and Living Animals
                • Thillai V. Sekar
                • , 
                • Kira Foygel
                • , 
                • Rammohan Devulapally
                • , and 
                • Ramasamy Paulmurugan*
                ACS Chem. Biol. 2015, 10, 1, 165-174
                • Open Access
                Publication Date (Web):December 9, 2014
                Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a
                • Ramzi F. Sweis*
                • , 
                • Marina Pliushchev
                • , 
                • Peter J. Brown
                • , 
                • Jun Guo
                • , 
                • Fengling Li
                • , 
                • David Maag
                • , 
                • Andrew M. Petros
                • , 
                • Nirupama B. Soni
                • , 
                • Chris Tse
                • , 
                • Masoud Vedadi
                • , 
                • Michael R. Michaelides
                • , 
                • Gary G. Chiang
                • , and 
                • William N. Pappano
                ACS Med. Chem. Lett. 2014, 5, 2, 205-209
                  Publication Date (Web):January 2, 2014
                  Article figure
                  Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
                  • Feng Liu
                  • , 
                  • Dalia Barsyte-Lovejoy
                  • , 
                  • Fengling Li
                  • , 
                  • Yan Xiong
                  • , 
                  • Victoria Korboukh
                  • , 
                  • Xi-Ping Huang
                  • , 
                  • Abdellah Allali-Hassani
                  • , 
                  • William P. Janzen
                  • , 
                  • Bryan L. Roth
                  • , 
                  • Stephen V. Frye
                  • , 
                  • Cheryl H. Arrowsmith
                  • , 
                  • Peter J. Brown
                  • , 
                  • Masoud Vedadi
                  • , and 
                  • Jian Jin*
                  J. Med. Chem. 2013, 56, 21, 8931-8942
                    Publication Date (Web):October 8, 2013
                    Article figure
                    Bromodomains: Are Readers Right for Epigenetic Therapy?
                    • Stuart J. Conway*
                    ACS Med. Chem. Lett. 2012, 3, 9, 691-694
                    • Free to Read Access
                    Publication Date (Web):August 9, 2012
                    Article figure
                    Mass Spectrometry-Based Detection and Assignment of Protein Posttranslational Modifications
                    • Sophia Doll
                    •  and 
                    • Alma L. Burlingame*
                    ACS Chem. Biol. 2015, 10, 1, 63-71
                    • Open Access
                    Publication Date (Web):December 26, 2014
                    Article figure
                    Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3
                    • Lindsey I. James
                    • , 
                    • Victoria K. Korboukh
                    • , 
                    • Liubov Krichevsky
                    • , 
                    • Brandi M. Baughman
                    • , 
                    • J. Martin Herold
                    • , 
                    • Jacqueline L. Norris
                    • , 
                    • Jian Jin
                    • , 
                    • Dmitri B. Kireev
                    • , 
                    • William P. Janzen
                    • , 
                    • Cheryl H. Arrowsmith
                    • , and 
                    • Stephen V. Frye*
                    J. Med. Chem. 2013, 56, 18, 7358-7371
                      Publication Date (Web):September 16, 2013
                      Article figure
                      Metabolic Regulation of Histone Post-Translational Modifications
                      • Jing Fan
                      • , 
                      • Kimberly A. Krautkramer
                      • , 
                      • Jessica L. Feldman
                      • , and 
                      • John M. Denu*
                      ACS Chem. Biol. 2015, 10, 1, 95-108
                      • Free to Read Access
                      Publication Date (Web):January 6, 2015
                      Article figure
                      Most Methylation-Susceptible DNA Sequences in Human Embryonic Stem Cells Undergo a Change in Conformation or Flexibility upon Methylation
                      • Yasutoshi Shimooka
                      • , 
                      • Jun-ichi Nishikawa
                      • , and 
                      • Takashi Ohyama*
                      Biochemistry 2013, 52, 8, 1344-1353
                        Publication Date (Web):January 28, 2013
                        Article figure
                        Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors
                        • Victor S. Gehling*
                        • , 
                        • Michael C. Hewitt*
                        • , 
                        • Rishi G. Vaswani
                        • , 
                        • Yves Leblanc
                        • , 
                        • Alexandre Côté
                        • , 
                        • Christopher G. Nasveschuk
                        • , 
                        • Alexander M. Taylor
                        • , 
                        • Jean-Christophe Harmange
                        • , 
                        • James E. Audia
                        • , 
                        • Eneida Pardo
                        • , 
                        • Shivangi Joshi
                        • , 
                        • Peter Sandy
                        • , 
                        • Jennifer A. Mertz
                        • , 
                        • Robert J. Sims III
                        • , 
                        • Louise Bergeron
                        • , 
                        • Barbara M. Bryant
                        • , 
                        • Steve Bellon
                        • , 
                        • Florence Poy
                        • , 
                        • Hariharan Jayaram
                        • , 
                        • Ravichandran Sankaranarayanan
                        • , 
                        • Sreegouri Yellapantula
                        • , 
                        • Nandana Bangalore Srinivasamurthy
                        • , 
                        • Swarnakumari Birudukota
                        • , and 
                        • Brian K. Albrecht
                        ACS Med. Chem. Lett. 2013, 4, 9, 835-840
                          Publication Date (Web):July 16, 2013
                          Article figure
                          Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors
                          • Feng Liu
                          • , 
                          • Fengling Li
                          • , 
                          • Anqi Ma
                          • , 
                          • Elena Dobrovetsky
                          • , 
                          • Aiping Dong
                          • , 
                          • Cen Gao
                          • , 
                          • Ilia Korboukh
                          • , 
                          • Jing Liu
                          • , 
                          • David Smil
                          • , 
                          • Peter J. Brown
                          • , 
                          • Stephen V. Frye
                          • , 
                          • Cheryl H. Arrowsmith
                          • , 
                          • Matthieu Schapira
                          • , 
                          • Masoud Vedadi*
                          • , and 
                          • Jian Jin*
                          J. Med. Chem. 2013, 56, 5, 2110-2124
                            Publication Date (Web):February 27, 2013
                            Article figure
                            Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions
                            • Michael Brand
                            • , 
                            • Angelina M. Measures
                            • , 
                            • Brian G. Wilson
                            • , 
                            • Wilian A. Cortopassi
                            • , 
                            • Rikki Alexander
                            • , 
                            • Matthias Höss
                            • , 
                            • David S. Hewings
                            • , 
                            • Timothy P. C. Rooney
                            • , 
                            • Robert S. Paton
                            • , and 
                            • Stuart J. Conway*
                            ACS Chem. Biol. 2015, 10, 1, 22-39
                            • Free to Read Access
                            Publication Date (Web):December 30, 2014
                            Article figure
                            Levuglandin Forms Adducts with Histone H4 in a Cyclooxygenase-2-Dependent Manner, Altering Its Interaction with DNA
                            • Erica J. Carrier
                            • , 
                            • Irene Zagol-Ikapitte
                            • , 
                            • Venkataraman Amarnath
                            • , 
                            • Olivier Boutaud*
                            • , and 
                            • John A. Oates
                            Biochemistry 2014, 53, 15, 2436-2441
                            • Open Access
                            Publication Date (Web):March 31, 2014
                            Article figure
                            Inhibitors of the NAD+-Dependent Protein Desuccinylase and Demalonylase Sirt5
                            • Benjamin Maurer
                            • , 
                            • Tobias Rumpf
                            • , 
                            • Michael Scharfe
                            • , 
                            • Diana A. Stolfa
                            • , 
                            • Martin L. Schmitt
                            • , 
                            • Wenjuan He
                            • , 
                            • Eric Verdin
                            • , 
                            • Wolfgang Sippl
                            • , and 
                            • Manfred Jung*
                            ACS Med. Chem. Lett. 2012, 3, 12, 1050-1053
                              Publication Date (Web):October 6, 2012
                              Article figure
                              Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
                              • David S. Hewings
                              • , 
                              • Oleg Fedorov
                              • , 
                              • Panagis Filippakopoulos
                              • , 
                              • Sarah Martin
                              • , 
                              • Sarah Picaud
                              • , 
                              • Anthony Tumber
                              • , 
                              • Christopher Wells
                              • , 
                              • Monica M. Olcina
                              • , 
                              • Katherine Freeman
                              • , 
                              • Andrew Gill
                              • , 
                              • Alison J. Ritchie
                              • , 
                              • David W. Sheppard
                              • , 
                              • Angela J. Russell
                              • , 
                              • Ester M. Hammond
                              • , 
                              • Stefan Knapp
                              • , 
                              • Paul E. Brennan
                              • , and 
                              • Stuart J. Conway*
                              J. Med. Chem. 2013, 56, 8, 3217-3227
                              • Open Access
                              Publication Date (Web):March 21, 2013
                              Article figure
                              Epigenetic Modification, Dehydration, and Molecular Crowding Effects on the Thermodynamics of i-Motif Structure Formation from C-Rich DNA
                              • Yogini P. Bhavsar-Jog
                              • , 
                              • Eric Van Dornshuld
                              • , 
                              • Tracy A. Brooks
                              • , 
                              • Gregory S. Tschumper
                              • , and 
                              • Randy M. Wadkins*
                              Biochemistry 2014, 53, 10, 1586-1594
                              • Open Access
                              Publication Date (Web):February 24, 2014
                              Article figure
                              Triazole–Dithiocarbamate Based Selective Lysine Specific Demethylase 1 (LSD1) Inactivators Inhibit Gastric Cancer Cell Growth, Invasion, and Migration
                              • Yi-Chao Zheng
                              • , 
                              • Ying-Chao Duan
                              • , 
                              • Jin-Lian Ma
                              • , 
                              • Rui-Min Xu
                              • , 
                              • Xiaolin Zi
                              • , 
                              • Wen-Lei Lv
                              • , 
                              • Meng-Meng Wang
                              • , 
                              • Xian-Wei Ye
                              • , 
                              • Shun Zhu
                              • , 
                              • David Mobley
                              • , 
                              • Yan-Yan Zhu
                              • , 
                              • Jun-Wei Wang
                              • , 
                              • Jin-Feng Li
                              • , 
                              • Zhi-Ru Wang
                              • , 
                              • Wen Zhao
                              • , and 
                              • Hong-Min Liu*
                              J. Med. Chem. 2013, 56, 21, 8543-8560
                                Publication Date (Web):October 16, 2013
                                Article figure
                                Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor
                                • Emily Borretto
                                • , 
                                • Loretta Lazzarato
                                • , 
                                • Francesco Spallotta
                                • , 
                                • Chiara Cencioni
                                • , 
                                • Yuri D’Alessandra
                                • , 
                                • Carlo Gaetano
                                • , 
                                • Roberta Fruttero*
                                • , and 
                                • Alberto Gasco
                                ACS Med. Chem. Lett. 2013, 4, 10, 994-999
                                  Publication Date (Web):September 4, 2013

                                  Virtual Collections

                                  Previously published research on topics of current scientific interest.

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