Chromatin proteins and modifications as drug targets

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

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

Bromo-deaza-SAH: A potent and selective DOT1L inhibitor

(2013) Wenyu Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

EZH2 Is Required for Germinal Center Formation and Somatic EZH2 Mutations Promote Lymphoid Transformation

(2013) Wendy Béguelin et al.   CANCER CELL

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

(2013) S. Picaud et al.   CANCER RESEARCH

Three-dimensional culture sensitizes epithelial ovarian cancer cells to EZH2 methyltransferase inhibition

(2013) Michael Amatangelo et al.   CELL CYCLE

Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors

(2013) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

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

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

(2013) S. K. Knutson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of PRC2 Activity by a Gain-of-Function H3 Mutation Found in Pediatric Glioblastoma

(2013) P. W. Lewis et al.   SCIENCE

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition

(2013) Alexandre Puissant et al.   Cancer Discovery

A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma

(2012) Yuan Yuan et al.   ACS Chemical Biology

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

(2012) Sergio Valente et al.   BIOCHIMIE

Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

(2012) Jonathan Seal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Histone Demethylase KDM1A Sustains the Oncogenic Potential of MLL-AF9 Leukemia Stem Cells

(2012) William J. Harris et al.   CANCER CELL

Cancer Genetics and Epigenetics: Two Sides of the Same Coin?

(2012) Jueng Soo You et al.   CANCER CELL

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

(2012) Panagis Filippakopoulos et al.   CELL

LSD1 inhibition: a therapeutic strategy in cancer?

(2012) James T Lynch et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

A key role for EZH2 and associated genes in mouse and human adult T-cell acute leukemia

(2012) C. Simon et al.   GENES & DEVELOPMENT

Synthesis and Structure–Activity Relationship Investigation of Adenosine-Containing Inhibitors of Histone Methyltransferase DOT1L

(2012) Justin L. Anglin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel mutations target distinct subgroups of medulloblastoma

(2012) Giles Robinson 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

The genetic basis of early T-cell precursor acute lymphoblastic leukaemia

(2012) Jinghui Zhang et al.   NATURE

Genetic inactivation of the polycomb repressive complex 2 in T cell acute lymphoblastic leukemia

(2012) Panagiotis Ntziachristos et al.   NATURE MEDICINE

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

Complexities of occupancy and sequence

(2012) Mary Muers   NATURE REVIEWS GENETICS

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

(2012) M. T. McCabe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

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

Genetic Events That Shape the Cancer Epigenome

(2012) R. J. H. Ryan et al.   SCIENCE

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Structural basis for CARM1 inhibition by indole and pyrazole inhibitors

(2011) John S. Sack et al.   BIOCHEMICAL JOURNAL

KDM2b/JHDM1b, an H3K36me2-specific demethylase, is required for initiation and maintenance of acute myeloid leukemia

(2011) J. He et al.   BLOOD

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

(2011) Kathrin M. Bernt et al.   CANCER CELL

HDAC4-Regulated STAT1 Activation Mediates Platinum Resistance in Ovarian Cancer

(2011) E. A. Stronach et al.   CANCER RESEARCH

Validation of the histone methyltransferase EZH2 as a therapeutic target for various types of human cancer and as a prognostic marker

(2011) Masashi Takawa et al.   CANCER SCIENCE

Combinatorial Patterning of Chromatin Regulators Uncovered by Genome-wide Location Analysis in Human Cells

(2011) Oren Ram et al.   CELL

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

(2011) Jake E. Delmore et al.   CELL

HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

(2011) Omar Khan et al.   IMMUNOLOGY AND CELL BIOLOGY

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

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

Role of androgen receptor and associated lysine-demethylase coregulators, LSD1 and JMJD2A, in localized and advanced human bladder cancer

(2011) Eric C. Kauffman et al.   MOLECULAR CARCINOGENESIS

NSD2 Links Dimethylation of Histone H3 at Lysine 36 to Oncogenic Programming

(2011) Alex J. Kuo et al.   MOLECULAR CELL

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

(2011) Mark A. Dawson et al.   NATURE

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Analysis of the coding genome of diffuse large B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE GENETICS

EZH2 Codon 641 Mutations are Common in BCL2-Rearranged Germinal Center B Cell Lymphomas

(2011) Russell J. H. Ryan et al.   PLoS One

Reversal of Histone Methylation: Biochemical and Molecular Mechanisms of Histone Demethylases

(2010) Nima Mosammaparast et al.   Annual Review of Biochemistry

Enhancer of zeste homolog 2 (EZH2) expression is an independent prognostic factor in renal cell carcinoma

(2010) Nina Wagener et al.   BMC CANCER

Overexpression of LSD1 contributes to human carcinogenesis through chromatin regulation in various cancers

(2010) Shinya Hayami et al.   INTERNATIONAL JOURNAL OF CANCER

Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.

(2010) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overexpression of the JmjC histone demethylase KDM5B in human carcinogenesis: involvement in the proliferation of cancer cells through the E2F/RB pathway

(2010) Shinya Hayami et al.   Molecular Cancer

Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

(2010) Gillian L. Dalgliesh et al.   NATURE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes

(2010) Gorica Nikoloski et al.   NATURE GENETICS

Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin

(2010) Ryan D Morin et al.   NATURE GENETICS

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

(2010) Thomas Ernst et al.   NATURE GENETICS

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

(2010) C. J. Sneeringer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Polycomb group protein-mediated repression of transcription

(2010) Lluís Morey et al.   TRENDS IN BIOCHEMICAL SCIENCES

Targeting DNA methylation for epigenetic therapy

(2010) Xiaojing Yang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Histone deacetylase (HDAC) inhibitors in recent clinical trials for cancer therapy

(2010) Julia M. Wagner et al.   Clinical Epigenetics

The chromatin-targeting protein Brd2 is required for neural tube closure and embryogenesis

(2009) Aron Gyuris et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)—Hit to Lead studies

(2009) Honghe Wan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Lysine-Specific Demethylase 1 Is Strongly Expressed in Poorly Differentiated Neuroblastoma: Implications for Therapy

(2009) J. H. Schulte et al.   CANCER RESEARCH

Targeting DNA Methylation

(2009) J.-P. J. Issa et al.   CLINICAL CANCER RESEARCH

New insights to the MLL recombinome of acute leukemias

(2009) C Meyer et al.   LEUKEMIA

DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation

(2009) T. B. Miranda et al.   MOLECULAR CANCER THERAPEUTICS

Minireview: Role of Protein Methylation and Demethylation in Nuclear Hormone Signaling

(2009) Susan C. Wu et al.   MOLECULAR ENDOCRINOLOGY

Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer

(2009) Gijs van Haaften et al.   NATURE GENETICS

Inhibition of the histone demethylase LSD1 blocks α-herpesvirus lytic replication and reactivation from latency

(2009) Yu Liang et al.   NATURE MEDICINE

Genomic amplification and oncogenic properties of the GASC1 histone demethylase gene in breast cancer

(2009) G Liu et al.   ONCOGENE

N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1)

(2008) Martin Allan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Demystified molecular pathology of NUT midline carcinomas

(2008) C. A. French   JOURNAL OF CLINICAL PATHOLOGY