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

The Role of Phase Separation in Heterochromatin Formation, Function, and Regulation

(2018) Adam G. Larson et al.   BIOCHEMISTRY

Functional Implications of Intracellular Phase Transitions

(2018) Alex S. Holehouse et al.   BIOCHEMISTRY

Formation of Chromatin Subcompartments by Phase Separation

(2018) Fabian Erdel et al.   BIOPHYSICAL JOURNAL

ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia

(2018) Tamara Maes et al.   CANCER CELL

A Phase I Clinical Trial of Guadecitabine and Carboplatin in Platinum-Resistant, Recurrent Ovarian Cancer: Clinical, Pharmacokinetic, and Pharmacodynamic Analyses

(2018) Daniela Matei et al.   CLINICAL CANCER RESEARCH

Lenalidomide plus dexamethasone for patients with relapsed or refractory multiple myeloma: Final results of a non-interventional study and comparison with the pivotal phase 3 clinical trials

(2018) Wolfgang Knauf et al.   LEUKEMIA RESEARCH

The dTAG system for immediate and target-specific protein degradation

(2018) Behnam Nabet et al.   Nature Chemical Biology

Chemically induced proximity in biology and medicine

(2018) Benjamin Z. Stanton et al.   SCIENCE

Imaging dynamic and selective low-complexity domain interactions that control gene transcription

(2018) Shasha Chong et al.   SCIENCE

Coactivator condensation at super-enhancers links phase separation and gene control

(2018) Benjamin R. Sabari et al.   SCIENCE

Mediator and RNA polymerase II clusters associate in transcription-dependent condensates

(2018) Won-Ki Cho et al.   SCIENCE

TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma

(2018) Kazuhide Nakayama et al.   Oncotarget

Intrinsically disordered sequences enable modulation of protein phase separation through distributed tyrosine motifs

(2017) Yuan Lin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe

(2017) Philip G. Humphreys et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemically Controlled Epigenome Editing through an Inducible dCas9 System

(2017) Tingjun Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Engineered Split-TET2 Enzyme for Inducible Epigenetic Remodeling

(2017) Minjung Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inducible Caspase-9 Selectively Modulates the Toxicities of CD19-Specific Chimeric Antigen Receptor-Modified T Cells

(2017) Iulia Diaconu et al.   MOLECULAR THERAPY

Molecular biology: A liquid reservoir for silent chromatin

(2017) Adam Klosin et al.   NATURE

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

(2017) Loren M. Lasko et al.   NATURE

Phase separation drives heterochromatin domain formation

(2017) Amy R. Strom et al.   NATURE

Liquid droplet formation by HP1α suggests a role for phase separation in heterochromatin

(2017) Adam G. Larson et al.   NATURE

Human antibody-based chemically induced dimerizers for cell therapeutic applications

(2017) Zachary B Hill et al.   Nature Chemical Biology

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

(2017) Yupeng He et al.   Nature Chemical Biology

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

(2017) Kenneth D Bromberg et al.   Nature Chemical Biology

Biomolecular condensates: organizers of cellular biochemistry

(2017) Salman F. Banani et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Dominant-negative SMARCA4 mutants alter the accessibility landscape of tissue-unrestricted enhancers

(2017) H. Courtney Hodges et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

TOP2 synergizes with BAF chromatin remodeling for both resolution and formation of facultative heterochromatin

(2017) Erik L Miller et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Liquid phase condensation in cell physiology and disease

(2017) Yongdae Shin et al.   SCIENCE

Rapid and reversible epigenome editing by endogenous chromatin regulators

(2017) Simon M. G. Braun et al.   Nature Communications

Identification of the elementary structural units of the DNA damage response

(2017) Francesco Natale et al.   Nature Communications

Dominant-negative SMARCA4 mutants alter the accessibility landscape of tissue-unrestricted enhancers

(2017) H. Courtney Hodges et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

TOP2 synergizes with BAF chromatin remodeling for both resolution and formation of facultative heterochromatin

(2017) Erik L Miller et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Intrinsically disordered linkers determine the interplay between phase separation and gelation in multivalent proteins

(2017) Tyler S Harmon et al.   eLife

Discovery of a PCAF Bromodomain Chemical Probe

(2016) Moses Moustakim et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Chemical Probe for the ATAD2 Bromodomain

(2016) Paul Bamborough et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112

(2016) Beth E. Zucconi et al.   BIOCHEMISTRY

N-Myc Induces an EZH2-Mediated Transcriptional Program Driving Neuroendocrine Prostate Cancer

(2016) Etienne Dardenne et al.   CANCER CELL

Mechanisms and Consequences of Macromolecular Phase Separation

(2016) Louis-Philippe Bergeron-Sandoval et al.   CELL

Live Cell Imaging Reveals the Dynamics of Telomerase Recruitment to Telomeres

(2016) Jens C. Schmidt et al.   CELL

Coexisting Liquid Phases Underlie Nucleolar Subcompartments

(2016) Marina Feric et al.   CELL

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

(2016) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cause and Consequence of Tethering a SubTAD to Different Nuclear Compartments

(2016) Patrick J. Wijchers et al.   MOLECULAR CELL

Sequence Determinants of Intracellular Phase Separation by Complex Coacervation of a Disordered Protein

(2016) Chi W. Pak et al.   MOLECULAR CELL

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

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

Smarca4 ATPase mutations disrupt direct eviction of PRC1 from chromatin

(2016) Benjamin Z Stanton et al.   NATURE GENETICS

Bright photoactivatable fluorophores for single-molecule imaging

(2016) Jonathan B Grimm et al.   NATURE METHODS

Spatial organization of chromatin domains and compartments in single chromosomes

(2016) Siyuan Wang et al.   SCIENCE

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

(2016) Paul Bamborough et al.   ACS Medicinal Chemistry Letters

Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7

(2016) Chunyan Ren et al.   ACS Medicinal Chemistry Letters

The Many Roles of BAF (mSWI/SNF) and PBAF Complexes in Cancer

(2016) Courtney Hodges et al.   Cold Spring Harbor Perspectives in Medicine

HDACs and HDAC Inhibitors in Cancer Development and Therapy

(2016) Yixuan Li et al.   Cold Spring Harbor Perspectives in Medicine

Distinct stages in stress granule assembly and disassembly

(2016) Joshua R Wheeler et al.   eLife

Small Molecules Modulate Chromatin Accessibility to Promote NEUROG2-Mediated Fibroblast-to-Neuron Reprogramming

(2016) Derek K. Smith et al.   Stem Cell Reports

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

(2015) Dennis L. Buckley et al.   ACS Chemical Biology

RAD1901

(2015) Fiona Garner et al.   ANTI-CANCER DRUGS

HaloTag Technology: A Versatile Platform for Biomedical Applications

(2015) Christopher G. England et al.   BIOCONJUGATE CHEMISTRY

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL

(2015) P. R. Hagner et al.   BLOOD

Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo

(2015) Dmitry Borkin et al.   CANCER CELL

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

(2015) Helai P. Mohammad et al.   CANCER CELL

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

(2015) Bhavatarini Vangamudi et al.   CANCER RESEARCH

Phase Separation by Low Complexity Domains Promotes Stress Granule Assembly and Drives Pathological Fibrillization

(2015) Amandine Molliex et al.   CELL

A Liquid-to-Solid Phase Transition of the ALS Protein FUS Accelerated by Disease Mutation

(2015) Avinash Patel et al.   CELL

Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G

(2015) Zibo Zhao et al.   CHEMISTRY & BIOLOGY

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

(2015) Chunyan Ren et al.   CHEMISTRY & BIOLOGY

FDA Approval: Belinostat for the Treatment of Patients with Relapsed or Refractory Peripheral T-cell Lymphoma

(2015) H.-Z. Lee et al.   CLINICAL CANCER RESEARCH

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

Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts

(2015) Andiliy Lai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and tolerability of guadecitabine (SGI-110) in patients with myelodysplastic syndrome and acute myeloid leukaemia: a multicentre, randomised, dose-escalation phase 1 study

(2015) Jean-Pierre J Issa et al.   LANCET ONCOLOGY

Imaging Live-Cell Dynamics and Structure at the Single-Molecule Level

(2015) Zhe Liu et al.   MOLECULAR CELL

Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents

(2015) Madhusoodanan Mottamal et al.   MOLECULES

Tunable and reversible drug control of protein production via a self-excising degron

(2015) Hokyung K Chung et al.   Nature Chemical Biology

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

(2015) Florian Grebien et al.   Nature Chemical Biology

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

A general method to improve fluorophores for live-cell and single-molecule microscopy

(2015) Jonathan B Grimm et al.   NATURE METHODS

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

iAID: an improved auxin-inducible degron system for the construction of a ‘tight’ conditional mutant in the budding yeastSaccharomyces cerevisiae

(2015) Seiji Tanaka et al.   YEAST

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

(2015) Kenneth W. Duncan et al.   ACS Medicinal Chemistry Letters

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat

(2015) James S. Scott et al.   ACS Medicinal Chemistry Letters

Targeting p300 Addiction in CBP-Deficient Cancers Causes Synthetic Lethality by Apoptotic Cell Death due to Abrogation of MYC Expression

(2015) H. Ogiwara et al.   Cancer Discovery

Promiscuous interactions and protein disaggregases determine the material state of stress-inducible RNP granules

(2015) Sonja Kroschwald et al.   eLife

Liquid-Liquid Phase Separation in Biology

(2014) Anthony A. Hyman et al.   Annual Review of Cell and Developmental Biology

A Phase II trial of Belinostat (PXD101) in patients with relapsed or refractory peripheral or cutaneous T-cell lymphoma

(2014) Francine Foss et al.   BRITISH JOURNAL OF HAEMATOLOGY

Single-Molecule Dynamics of Enhanceosome Assembly in Embryonic Stem Cells

(2014) Jiji Chen et al.   CELL

A 3D Map of the Human Genome at Kilobase Resolution Reveals Principles of Chromatin Looping

(2014) Suhas S.P. Rao et al.   CELL

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

(2014) Shihan He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chromodomain Antagonists That Target the Polycomb-Group Methyllysine Reader Protein Chromobox Homolog 7 (CBX7)

(2014) Chakravarthi Simhadri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Panobinostat plus bortezomib and dexamethasone versus placebo plus bortezomib and dexamethasone in patients with relapsed or relapsed and refractory multiple myeloma: a multicentre, randomised, double-blind phase 3 trial

(2014) Jesús F San-Miguel et al.   LANCET ONCOLOGY

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

(2014) S. K. Knutson et al.   MOLECULAR CANCER THERAPEUTICS

Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia

(2014) Fang Cao et al.   MOLECULAR CELL

Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia

(2014) Panagiotis Ntziachristos et al.   NATURE

Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma

(2014) Rintaro Hashizume et al.   NATURE MEDICINE

3D live fluorescence imaging of cellular dynamics using Bessel beam plane illumination microscopy

(2014) Liang Gao et al.   Nature Protocols

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

(2014) D. Barsyte-Lovejoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A rationale to target the SWI/SNF complex for cancer therapy

(2014) Anja F. Hohmann et al.   TRENDS IN GENETICS

Localized light-induced protein dimerization in living cells using a photocaged dimerizer

(2014) Edward R. Ballister et al.   Nature Communications

Therapeutic Strategies to Inhibit MYC

(2014) M. R. McKeown et al.   Cold Spring Harbor Perspectives in Medicine

A Hexylchloride-Based Catch-and-Release System for Chemical Proteomic Applications

(2013) Jennifer L. Brigham et al.   ACS Chemical Biology

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

(2013) Kyle D. Konze et al.   ACS Chemical Biology

Histone deacetylase inhibitors

(2013) Marije Slingerland et al.   ANTI-CANCER DRUGS

Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer

(2013) Robert H. Bradbury et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chemical Development of Intracellular Protein Heterodimerizers

(2013) Dominik Erhart et al.   CHEMISTRY & BIOLOGY

Cullin-RING Ligases as Attractive Anti-cancer Targets

(2013) Yongchao Zhao et al.   CURRENT PHARMACEUTICAL DESIGN

Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes

(2013) Brianna J Klein et al.   Epigenetics

A Small Molecule Inhibitor of Polycomb Repressive Complex 1 Inhibits Ubiquitin Signaling at DNA Double-strand Breaks

(2013) Ismail Hassan Ismail et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Stress granules as crucibles of ALS pathogenesis

(2013) Yun R. Li et al.   JOURNAL OF CELL BIOLOGY

Pomalidomide plus low-dose dexamethasone versus high-dose dexamethasone alone for patients with relapsed and refractory multiple myeloma (MM-003): a randomised, open-label, phase 3 trial

(2013) Jesus San Miguel et al.   LANCET ONCOLOGY

AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function In Vitro and In Vivo

(2013) S. A. Loddick et al.   MOLECULAR CANCER THERAPEUTICS

BAF complexes facilitate decatenation of DNA by topoisomerase IIα

(2013) Emily C. Dykhuizen et al.   NATURE

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

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

Real-Time Dynamics of RNA Polymerase II Clustering in Live Human Cells

(2013) I. I. Cisse et al.   SCIENCE

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

Small molecules enable neurogenin 2 to efficiently convert human fibroblasts into cholinergic neurons

(2013) Meng-Lu Liu et al.   Nature Communications

Estrogen and Cancer

(2012) Jing Liang et al.   Annual Review of Physiology

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

(2012) L. Santo et al.   BLOOD

Dynamics and Memory of Heterochromatin in Living Cells

(2012) Nathaniel A. Hathaway et al.   CELL

Three-Dimensional Folding and Functional Organization Principles of the Drosophila Genome

(2012) Tom Sexton et al.   CELL

Transcriptional Amplification in Tumor Cells with Elevated c-Myc

(2012) Charles Y. Lin et al.   CELL

Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface

(2012) Inge Van Molle et al.   CHEMISTRY & BIOLOGY

The Therapeutic Target Hsp90 and Cancer Hallmarks

(2012) Yoshihiko Miyata et al.   CURRENT PHARMACEUTICAL DESIGN

Doxorubicin: an update on anticancer molecular action, toxicity and novel drug delivery systems

(2012) Oktay Tacar et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Phase transitions in the assembly of multivalent signalling proteins

(2012) Pilong Li et al.   NATURE

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

Topological domains in mammalian genomes identified by analysis of chromatin interactions

(2012) Jesse R. Dixon et al.   NATURE

Epigenetic protein families: a new frontier for drug discovery

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

Nuclear receptor coregulators: modulators of pathology and therapeutic targets

(2012) David M. Lonard et al.   Nature Reviews Endocrinology

Dynamics of inherently bounded histone modification domains

(2012) C. Hodges et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inducible, reversible system for the rapid and complete degradation of proteins in mammalian cells

(2012) A. J. Holland et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer

(2011) Robert H. Bradbury et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A view of nuclear Polycomb bodies

(2011) Vincenzo Pirrotta et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

P granules extend the nuclear pore complex environment in theC. elegansgerm line

(2011) Dustin L. Updike et al.   JOURNAL OF CELL BIOLOGY

Inhibition of the Acetyltransferases p300 and CBP Reveals a Targetable Function for p300 in the Survival and Invasion Pathways of Prostate Cancer Cell Lines

(2011) F. R. Santer et al.   MOLECULAR CANCER THERAPEUTICS

Rapid three-dimensional isotropic imaging of living cells using Bessel beam plane illumination

(2011) Thomas A Planchon et al.   NATURE METHODS

The Leukemogenicity of AML1-ETO Is Dependent on Site-Specific Lysine Acetylation

(2011) L. Wang et al.   SCIENCE

Engineering the ABA Plant Stress Pathway for Regulation of Induced Proximity

(2011) F.-S. Liang et al.   Science Signaling

Targeting heat shock proteins in cancer

(2010) Gaëtan Jego et al.   CANCER LETTERS

Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor

(2010) Erin M. Bowers et al.   CHEMISTRY & BIOLOGY

DNA Topoisomerases and Their Poisoning by Anticancer and Antibacterial Drugs

(2010) Yves Pommier et al.   CHEMISTRY & BIOLOGY

Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen

(2010) Naomi Suzuki et al.   INTERNATIONAL JOURNAL OF CANCER

Final Results From a Multicenter, International, Pivotal Study of Romidepsin in Refractory Cutaneous T-Cell Lymphoma

(2010) Sean J. Whittaker et al.   JOURNAL OF CLINICAL ONCOLOGY

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

S110, a 5-Aza-2'-Deoxycytidine-Containing Dinucleotide, Is an Effective DNA Methylation Inhibitor In vivo and Can Reduce Tumor Growth

(2010) J. C. Chuang et al.   MOLECULAR CANCER THERAPEUTICS

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

BRD7 is a candidate tumour suppressor gene required for p53 function

(2010) Jarno Drost et al.   NATURE CELL BIOLOGY

Direct visualization of the co-transcriptional assembly of a nuclear body by noncoding RNAs

(2010) Yuntao S. Mao et al.   NATURE CELL BIOLOGY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Epigenetic Dysregulation in Cancer

(2009) Andrew G. Muntean et al.   AMERICAN JOURNAL OF PATHOLOGY

The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene expression in acute myeloid leukemia cells

(2009) C Flotho et al.   LEUKEMIA

An auxin-based degron system for the rapid depletion of proteins in nonplant cells

(2009) Kohei Nishimura et al.   NATURE METHODS

Comprehensive Mapping of Long-Range Interactions Reveals Folding Principles of the Human Genome

(2009) E. Lieberman-Aiden et al.   SCIENCE

DNA methylation patterns in lung carcinomas

(2009) Gerd P. Pfeifer et al.   SEMINARS IN CANCER BIOLOGY

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Anacardic acid (6-nonadecyl salicylic acid), an inhibitor of histone acetyltransferase, suppresses expression of nuclear factor- B-regulated gene products involved in cell survival, proliferation, invasion, and inflammation through inhibition of the inhibitory subunit of nuclear factor- B  kinase, leading to potentiation of apoptosis

(2008) B. Sung et al.   BLOOD

Long-term Epigenetic Therapy with Oral Zebularine Has Minimal Side Effects and Prevents Intestinal Tumors in Mice

(2008) C. B. Yoo et al.   Cancer Prevention Research

Targeting Hsp90: small-molecule inhibitors and their clinical development

(2008) Tony Taldone et al.   CURRENT OPINION IN PHARMACOLOGY

A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas

(2008) S Balasubramanian et al.   LEUKEMIA

Development of an Aryl Hydrocarbon Receptor Antagonist Using the Proteolysis-Targeting Chimeric Molecules Approach: A Potential Tool for Chemoprevention

(2008) D. Puppala et al.   MOLECULAR PHARMACOLOGY

Highly inclined thin illumination enables clear single-molecule imaging in cells

(2008) Makio Tokunaga et al.   NATURE METHODS

Topoisomerase II: a fitted mechanism for the chromatin landscape

(2008) J. Roca   NUCLEIC ACIDS RESEARCH