Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy

Solution structure of TbTFIIS2-2 PWWP domain from Trypanosoma brucei and its binding to H4K17me3 and H3K32me3

(2019) Rui Wang et al.   BIOCHEMICAL JOURNAL

Reading Cancer: Chromatin Readers as Druggable Targets for Cancer Treatment

(2019) Catia Mio et al.   Cancers

The HRP3 PWWP domain recognizes the minor groove of double-stranded DNA and recruits HRP3 to chromatin

(2019) Wei Tian et al.   NUCLEIC ACIDS RESEARCH

A DNMT3A PWWP mutation leads to methylation of bivalent chromatin and growth retardation in mice

(2019) Gintarė Sendžikaitė et al.   Nature Communications

The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases

(2019) Martin Roatsch et al.   ACS Chemical Biology

Selective binding of the PHD6 finger of MLL4 to histone H4K16ac links MLL4 and MOF

(2019) Yi Zhang et al.   Nature Communications

BET inhibitor bromosporine enhances 5-FU effect in colorectal cancer cells

(2019) Xueyuan Cheng et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor

(2019) Sijie Wang et al.   ACS Chemical Biology

Targeting Epigenetics in Cancer

(2018) Richard L. Bennett et al.   Annual Review of Pharmacology and Toxicology

Transcriptional and posttranscriptional repression of histone deacetylases by docosahexaenoic acid in macrophages

(2018) Tho X. Pham et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Affinity switching of the LEDGF/p75 IBD interactome is governed by kinase-dependent phosphorylation

(2018) Subhalakshmi Sharma et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GAS41 Recognizes Diacetylated Histone H3 through a Bivalent Binding Mode

(2018) Hyo Je Cho et al.   ACS Chemical Biology

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

(2018) Subhankar Biswas et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

SP140 regulates the expression of immune-related genes associated with multiple sclerosis and other autoimmune diseases by NF-κB inhibition

(2018) Mohamad Karaky et al.   HUMAN MOLECULAR GENETICS

Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation

(2018) Katerina Cermakova et al.   MOLECULES

Reading More than Histones: The Prevalence of Nucleic Acid Binding among Reader Domains

(2018) Tyler Weaver et al.   MOLECULES

Brd4’s Bromodomains Mediate Histone H3 Acetylation and Chromatin Remodeling in Pluripotent Cells through P300 and Brg1

(2018) Tao Wu et al.   Cell Reports

ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia

(2017) Liling Wan et al.   NATURE

WD40 repeat domain proteins: a novel target class?

(2017) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer

(2017) Takao Fujisawa et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Histone-binding of DPF2 mediates its repressive role in myeloid differentiation

(2017) Ferdinand M. Huber et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

DNA binding drives the association of BRG1/hBRM bromodomains with nucleosomes

(2017) Emma A. Morrison et al.   Nature Communications

TRIM24 is an oncogenic transcriptional co-activator of STAT3 in glioblastoma

(2017) Deguan Lv et al.   Nature Communications

Design, synthesis, and protein methyltransferase activity of a unique set of constrained amine containing compounds

(2016) Hao Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bromodomain inhibitors and cancer therapy: From structures to applications

(2016) Montserrat Pérez-Salvia et al.   Epigenetics

OTX015 (MK-8628), a novel BET inhibitor, displaysin vitroandin vivoantitumor effects alone and in combination with conventional therapies in glioblastoma models

(2016) Caroline Berenguer-Daizé et al.   INTERNATIONAL JOURNAL OF CANCER

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

(2016) Laetitia J. Martin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

(2016) Brian K. Albrecht et al.   JOURNAL OF MEDICINAL CHEMISTRY

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1

(2016) Jacob I Stuckey et al.   Nature Chemical Biology

Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition

(2016) Anja F Hohmann et al.   Nature Chemical Biology

Metabolic regulation of gene expression through histone acylations

(2016) Benjamin R. Sabari et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

ASH1L Links Histone H3 Lysine 36 Dimethylation to MLL Leukemia

(2016) L. Zhu et al.   Cancer Discovery

ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication

(2016) Seong Joo Koo et al.   Oncotarget

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin

(2016) Pavel Savitsky et al.   Cell Reports

Cbx8 Acts Non-canonically with Wdr5 to Promote Mammary Tumorigenesis

(2016) Chi-Yeh Chung et al.   Cell Reports

PHF20 Readers Link Methylation of Histone H3K4 and p53 with H4K16 Acetylation

(2016) Brianna J. Klein et al.   Cell Reports

Exploitation of EP300 and CREBBP Lysine Acetyltransferases by Cancer

(2016) Narsis Attar et al.   Cold Spring Harbor Perspectives in Medicine

Identification of a Fragment-like Small Molecule Ligand for the Methyl-lysine Binding Protein, 53BP1

(2015) Michael T. Perfetti et al.   ACS Chemical Biology

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial

(2015) Stephen J. Nicholls et al.   American Journal of Cardiovascular Drugs

Chemical Inhibitors of Epigenetic Methyllysine Reader Proteins

(2015) Natalia Milosevich et al.   BIOCHEMISTRY

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

(2015) S. Picaud et al.   CANCER RESEARCH

Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities

(2015) Eugene L. Piatnitski Chekler et al.   CHEMISTRY & BIOLOGY

Small-Molecule Modulators of Methyl-Lysine Binding for the CBX7 Chromodomain

(2015) Chunyan Ren et al.   CHEMISTRY & BIOLOGY

Natural compound-derived epigenetic regulators targeting epigenetic readers, writers and erasers

(2015) Anne Yuqing Yang et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

BRPF3-HBO1 regulates replication origin activation and histone H3K14 acetylation

(2015) Y. Feng et al.   EMBO JOURNAL

Structure and organization of chromatin fiber in the nucleus

(2015) Guohong Li et al.   FEBS LETTERS

Association of Taf14 with acetylated histone H3 directs gene transcription and the DNA damage response

(2015) Erin K. Shanle et al.   GENES & DEVELOPMENT

Molecular Insights into Inhibition of the Methylated Histone-Plant Homeodomain Complexes by Calixarenes

(2015) Muzaffar Ali et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

(2015) Natalie H. Theodoulou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors

(2015) F. Anthony Romero et al.   JOURNAL OF MEDICINAL CHEMISTRY

The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models

(2015) P L Garcia et al.   ONCOGENE

A Subset of Human Bromodomains Recognizes Butyryllysine and Crotonyllysine Histone Peptide Modifications

(2015) E. Megan Flynn et al.   STRUCTURE

Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family

(2015) Natalia Milosevich et al.   ACS Medicinal Chemistry Letters

Multiple cellular proteins interact with LEDGF/p75 through a conserved unstructured consensus motif

(2015) Petr Tesina et al.   Nature Communications

Competitive Binding of a Benzimidazole to the Histone-Binding Pocket of the Pygo PHD Finger

(2014) Thomas C. R. Miller et al.   ACS Chemical Biology

Binding Hotspots of BAZ2B Bromodomain: Histone Interaction Revealed by Solution NMR Driven Docking

(2014) Fleur M. Ferguson et al.   BIOCHEMISTRY

Validation and Structural Characterization of the LEDGF/p75-MLL Interface as a New Target for the Treatment of MLL-Dependent Leukemia

(2014) K.  ermakova et al.   CANCER RESEARCH

AF9 YEATS Domain Links Histone Acetylation to DOT1L-Mediated H3K79 Methylation

(2014) Yuanyuan Li et al.   CELL

A PWWP Domain-Containing Protein Targets the NuA3 Acetyltransferase Complex via Histone H3 Lysine 36 trimethylation to Coordinate Transcriptional Elongation at Coding Regions

(2014) Tonya M. Gilbert et al.   MOLECULAR & CELLULAR PROTEOMICS

Proteolytic clipping of histone tails: the emerging role of histone proteases in regulation of various biological processes

(2014) Gajendra Kumar Azad et al.   MOLECULAR BIOLOGY REPORTS

BS69/ZMYND11 Reads and Connects Histone H3.3 Lysine 36 Trimethylation-Decorated Chromatin to Regulated Pre-mRNA Processing

(2014) Rui Guo et al.   MOLECULAR CELL

Histone H3 phosphorylation near the nucleosome dyad alters chromatin structure

(2014) Justin A. North et al.   NUCLEIC ACIDS RESEARCH

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

Regulation of Transcription through Acetylation of H3K122 on the Lateral Surface of the Histone Octamer

(2013) Philipp Tropberger et al.   CELL

Targeting histone modifications—epigenetics in cancer

(2013) Tanja Waldmann et al.   CURRENT OPINION IN CELL BIOLOGY

The Malignant Brain Tumor (MBT) Domain Protein SFMBT1 Is an Integral Histone Reader Subunit of the LSD1 Demethylase Complex for Chromatin Association and Epithelial-to-mesenchymal Transition

(2013) Ming Tang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular Insights into the Recognition of N-Terminal Histone Modifications by the BRPF1 Bromodomain

(2013) Amanda Poplawski et al.   JOURNAL OF MOLECULAR BIOLOGY

Cdyl, a New Partner of the Inactive X Chromosome and Potential Reader of H3K27me3 and H3K9me2

(2013) M. Escamilla-Del-Arenal et al.   MOLECULAR AND CELLULAR BIOLOGY

Polycomb Cbx family members mediate the balance between haematopoietic stem cell self-renewal and differentiation

(2013) Karin Klauke et al.   NATURE CELL BIOLOGY

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

(2013) Lindsey I James et al.   Nature Chemical Biology

Molecular basis for chromatin binding and regulation of MLL5

(2013) M. Ali et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tudor: a versatile family of histone methylation ‘readers’

(2013) Rui Lu et al.   TRENDS IN BIOCHEMICAL SCIENCES

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition

(2013) Alexandre Puissant et al.   Cancer Discovery

Crosstalk between NSL Histone Acetyltransferase and MLL/SET Complexes: NSL Complex Functions in Promoting Histone H3K4 Di-Methylation Activity by MLL/SET Complexes

(2013) Xiaoming Zhao et al.   PLoS Genetics

Identification and Characterization of Small Molecule Inhibitors of a Plant Homeodomain Finger

(2012) Elise K. Wagner et al.   BIOCHEMISTRY

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

Nonoverlapping Functions of the Polycomb Group Cbx Family of Proteins in Embryonic Stem Cells

(2012) Lluis Morey et al.   Cell Stem Cell

Tudor domain proteins in development

(2012) J. W. Pek et al.   DEVELOPMENT

The p400/Brd8 Chromatin Remodeling Complex Promotes Adipogenesis by Incorporating Histone Variant H2A.Z at PPARγ Target Genes

(2012) Jean-Philippe Couture et al.   ENDOCRINOLOGY

Structural biology of the chromodomain: Form and function

(2012) Joel C. Eissenberg   GENE

Combinatorial readout of unmodified H3R2 and acetylated H3K14 by the tandem PHD finger of MOZ reveals a regulatory mechanism for HOXA9 transcription

(2012) Y. Qiu et al.   GENES & DEVELOPMENT

Tandem PHD Fingers of MORF/MOZ Acetyltransferases Display Selectivity for Acetylated Histone H3 and Are Required for the Association with Chromatin

(2012) Muzaffar Ali et al.   JOURNAL OF MOLECULAR BIOLOGY

An H3K36 Methylation-Engaging Tudor Motif of Polycomb-like Proteins Mediates PRC2 Complex Targeting

(2012) Ling Cai et al.   MOLECULAR CELL

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

Phf19 links methylated Lys36 of histone H3 to regulation of Polycomb activity

(2012) Cecilia Ballaré et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Molecular basis for H3K36me3 recognition by the Tudor domain of PHF1

(2012) Catherine A Musselman et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Perceiving the epigenetic landscape through histone readers

(2012) Catherine A Musselman et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

DNA Methylation and Its Basic Function

(2012) Lisa D Moore et al.   NEUROPSYCHOPHARMACOLOGY

Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins

(2012) W. W. Lockwood et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Place your BETs: the therapeutic potential of bromodomains

(2012) R.K. Prinjha et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Psip1/Ledgf p52 Binds Methylated Histone H3K36 and Splicing Factors and Contributes to the Regulation of Alternative Splicing

(2012) Madapura M. Pradeepa et al.   PLoS Genetics

Solution structure of the Pdp1 PWWP domain reveals its unique binding sites for methylated H4K20 and DNA

(2011) Yu Qiu et al.   BIOCHEMICAL JOURNAL

The Hbo1-Brd1/Brpf2 complex is responsible for global acetylation of H3K14 and required for fetal liver erythropoiesis

(2011) Y. Mishima et al.   BLOOD

CBX8, a Polycomb Group Protein, Is Essential for MLL-AF9-Induced Leukemogenesis

(2011) Jiaying Tan et al.   CANCER CELL

Recognition of a Mononucleosomal Histone Modification Pattern by BPTF via Multivalent Interactions

(2011) Alexander J. Ruthenburg et al.   CELL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

Plant Homeodomain (PHD) Fingers of CHD4 Are Histone H3-binding Modules with Preference for Unmodified H3K4 and Methylated H3K9

(2011) Robyn E. Mansfield et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

(2011) J. Martin Herold et al.   JOURNAL OF MEDICINAL CHEMISTRY

UHRF1 Double Tudor Domain and the Adjacent PHD Finger Act Together to Recognize K9me3-Containing Histone H3 Tail

(2011) Si Xie et al.   JOURNAL OF MOLECULAR BIOLOGY

Recruitment of TIF1γ to Chromatin via Its PHD Finger-Bromodomain Activates Its Ubiquitin Ligase and Transcriptional Repressor Activities

(2011) Eleonora Agricola et al.   MOLECULAR CELL

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Structural and Histone Binding Ability Characterizations of Human PWWP Domains

(2011) Hong Wu et al.   PLoS One

The PHD finger: a versatile epigenome reader

(2011) Roberto Sanchez et al.   TRENDS IN BIOCHEMICAL SCIENCES

H3K9me2/3 Binding of the MBT Domain Protein LIN-61 Is Essential for Caenorhabditis elegans Vulva Development

(2011) Nora Koester-Eiserfunke et al.   PLoS Genetics

Quantitative Interaction Proteomics and Genome-wide Profiling of Epigenetic Histone Marks and Their Readers

(2010) Michiel Vermeulen et al.   CELL

Keeping it in the family: diverse histone recognition by conserved structural folds

(2010) Kyoko L. Yap et al.   CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY

Distinct roles of GCN5/PCAF-mediated H3K9ac and CBP/p300-mediated H3K18/27ac in nuclear receptor transactivation

(2010) Qihuang Jin et al.   EMBO JOURNAL

PHD finger of autoimmune regulator: An epigenetic link between the histone modifications and tissue-specific antigen expression in thymus

(2010) Giovanna Musco et al.   Epigenetics

Recognition and Specificity Determinants of the Human Cbx Chromodomains

(2010) Lilia Kaustov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Chromatin Loading of E2F-MLL Complex by Cancer-Associated Coregulator ANCCA via Reading a Specific Histone Mark

(2010) A. S. Revenko et al.   MOLECULAR AND CELLULAR BIOLOGY

Loss, mutation and deregulation of L3MBTL4 in breast cancers

(2010) Lynda Addou-Klouche et al.   Molecular Cancer

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Genome-wide meta-analysis increases to 71 the number of confirmed Crohn's disease susceptibility loci

(2010) Andre Franke et al.   NATURE GENETICS

Corecognition of DNA and a methylated histone tail by the MSL3 chromodomain

(2010) Daesung Kim et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

YEATS domain proteins: a diverse family with many links to chromatin modification and transcriptionThis paper is one of a selection of papers published in this Special Issue, entitled CSBMCB’s 51st Annual Meeting – Epigenetics and Chromatin Dynamics, and has undergone the Journal’s usual peer review process.

(2009) Julia M. Schulze et al.   Biochemistry and Cell Biology

Genomic distribution of CHD7 on chromatin tracks H3K4 methylation patterns

(2009) M. P. Schnetz et al.   GENOME RESEARCH

Multimerization and H3K9me3 Binding Are Required for CDYL1b Heterochromatin Association

(2009) Henriette Franz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Regulation of Set9-Mediated H4K20 Methylation by a PWWP Domain Protein

(2009) Yu Wang et al.   MOLECULAR CELL

High-Affinity Binding of Chp1 Chromodomain to K9 Methylated Histone H3 Is Required to Establish Centromeric Heterochromatin

(2009) Thomas Schalch et al.   MOLECULAR CELL

Role of the polycomb protein EED in the propagation of repressive histone marks

(2009) Raphael Margueron et al.   NATURE

Cooperative binding of two acetylation marks on a histone tail by a single bromodomain

(2009) Jeanne Morinière et al.   NATURE

Enzymatic and structural insights for substrate specificity of a family of jumonji histone lysine demethylases

(2009) John R Horton et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Asf1-like structure of the conserved Yaf9 YEATS domain and role in H2A.Z deposition and acetylation

(2009) A. Y. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MBT domain proteins in development and disease

(2009) Roberto Bonasio et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Regulation of muscle development by DPF3, a novel histone acetylation and methylation reader of the BAF chromatin remodeling complex

(2008) M. Lange et al.   GENES & DEVELOPMENT

Balance between Distinct HP1 Family Proteins Controls Heterochromatin Assembly in Fission Yeast

(2008) M. Sadaie et al.   MOLECULAR AND CELLULAR BIOLOGY

The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription

(2008) Gary LeRoy et al.   MOLECULAR CELL

The many roles of histone deacetylases in development and physiology: implications for disease and therapy

(2008) Michael Haberland et al.   NATURE REVIEWS GENETICS

Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300

(2008) Lei Zeng et al.   STRUCTURE