Histone Lysine Demethylase Inhibitors

The histone demethylase LSD1 is a novel oncogene and therapeutic target in oral cancer

(2016) Yanling Wang et al.   CANCER LETTERS

UTX inhibition as selective epigenetic therapy against TAL1-driven T-cell acute lymphoblastic leukemia

(2016) Aissa Benyoucef et al.   GENES & DEVELOPMENT

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent

(2016) Paola Vianello et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone Demethylase LSD1 Inhibitors Prevent Cell Growth by Regulating Gene Expression in Esophageal Squamous Cell Carcinoma Cells

(2015) Isamu Hoshino et al.   ANNALS OF SURGICAL ONCOLOGY

Inhibition of LSD1 by Pargyline inhibited process of EMT and delayed progression of prostate cancer in vivo

(2015) Min Wang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Histone demethylase JARID1C promotes breast cancer metastasis cells via down regulating BRMS1 expression

(2015) Qin Wang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Structure–activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures

(2015) Shannon L. Nowotarski et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Histone H3 peptide based LSD1-selective inhibitors

(2015) Taeko Kakizawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Overexpression of the shortest isoform of histone demethylase LSD1 primes hematopoietic stem cells for malignant transformation

(2015) T. Wada et al.   BLOOD

Novel Tranylcypromine/Hydroxylcinnamic Acid Hybrids as Lysine-Specific Demethylase 1 Inhibitors with Potent Antitumor Activity

(2015) Yan Han et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes

(2015) Lingling Duan et al.   CHEMISTRY & BIOLOGY

Molecular Pathways: At the Crossroads of Cancer Epigenetics and Immunotherapy

(2015) M. Maio et al.   CLINICAL CANCER RESEARCH

Advances in the development of histone lysine demethylase inhibitors

(2015) Tamara Maes et al.   CURRENT OPINION IN PHARMACOLOGY

Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: Introduction of an additional carboxyl group at the C-2 position of quinoline

(2015) Taotao Feng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts

(2015) Sergio Valente et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases

(2015) John R. Horton et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1

(2015) Fangrui Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator

(2015) Li-Juan Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Structure–Activity Relationship of Novel LSD1 Inhibitors Based on Pyrimidine–Thiourea Hybrids As Potent, Orally Active Antitumor Agents

(2015) Li-Ying Ma et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Specific LSD1/KDM1A Isoform Regulates Neuronal Differentiation through H3K9 Demethylation

(2015) Benoit Laurent et al.   MOLECULAR CELL

LSD1n is an H4K20 demethylase regulating memory formation via transcriptional elongation control

(2015) Jianxun Wang et al.   NATURE NEUROSCIENCE

Design, synthesis, and biological activity of N-alkylated analogue of NCL1, a selective inhibitor of lysine-specific demethylase 1

(2015) Mohammed Naseer Ahmed Khan et al.   MedChemComm

Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells

(2015) Yukihiro Itoh et al.   ACS Medicinal Chemistry Letters

Lysine Demethylase KDM4A Associates with Translation Machinery and Regulates Protein Synthesis

(2015) C. Van Rechem et al.   Cancer Discovery

NCL1, a highly selective lysine-specific demethylase 1 inhibitor, suppresses prostate cancer without adverse effect

(2015) Toshiki Etani et al.   Oncotarget

KDM1 is a novel therapeutic target for the treatment of gliomas

(2015) Gangadhara R Sareddy et al.   Oncotarget

A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1

(2014) Polina Prusevich et al.   ACS Chemical Biology

Reversible inhibition of lysine specific demethylase 1 is a novel anti-tumor strategy for poorly differentiated endometrial carcinoma

(2014) Emily R Theisen et al.   BMC CANCER

Reconstructing and Reprogramming the Tumor-Propagating Potential of Glioblastoma Stem-like Cells

(2014) Mario L. Suvà et al.   CELL

A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1

(2014) Rachel Schiller et al.   ChemMedChem

Reversible LSD1 Inhibition Interferes with Global EWS/ETS Transcriptional Activity and Impedes Ewing Sarcoma Tumor Growth

(2014) S. Sankar et al.   CLINICAL CANCER RESEARCH

KDM4B as a Target for Prostate Cancer: Structural Analysis and Selective Inhibition by a Novel Inhibitor

(2014) Chia-Han Chu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells

(2014) W Fiskus et al.   LEUKEMIA

Inhibition of demethylases by GSK-J1/J4

(2014) Bo Heinemann et al.   NATURE

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

(2014) Panagiotis Ntziachristos et al.   NATURE

Synthesis and biological evaluation of hybrids from farnesylthiosalicylic acid and hydroxylcinnamic acid with dual inhibitory activities of Ras-related signaling and phosphorylated NF-κB

(2014) Yong Ling et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

An High-Throughput In Vivo Screening System to Select H3K4-Specific Histone Demethylase Inhibitors

(2014) Cecilia Mannironi et al.   PLoS One

Chem-seq permits identification of genomic targets of drugs against androgen receptor regulation selected by functional phenotypic screens

(2014) C. Jin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

(2014) Katherine S. England et al.   MedChemComm

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies

(2014) Sergio Valente et al.   ACS Medicinal Chemistry Letters

NUP98-PHF23 Is a Chromatin-Modifying Oncoprotein That Causes a Wide Array of Leukemias Sensitive to Inhibition of PHD Histone Reader Function

(2014) S. M. Gough et al.   Cancer Discovery

Suppression of Invasion and Metastasis of Triple-Negative Breast Cancer Lines by Pharmacological or Genetic Inhibition of Slug Activity

(2014) Giovanna Ferrari-Amorotti et al.   NEOPLASIA

Protein Recognition by Short Peptide Reversible Inhibitors of the Chromatin-Modifying LSD1/CoREST Lysine Demethylase

(2013) Marcello Tortorici et al.   ACS Chemical Biology

The re-expression of the epigenetically silenced e-cadherin gene by a polyamine analogue lysine-specific demethylase-1 (LSD1) inhibitor in human acute myeloid leukemia cell lines

(2013) Tracy Murray-Stewart et al.   AMINO ACIDS

The human flavoproteome

(2013) Wolf-Dieter Lienhart et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

LSD1-mediated epigenetic modification contributes to proliferation and metastasis of colon cancer

(2013) J Ding et al.   BRITISH JOURNAL OF CANCER

Crosstalk between lysine-specific demethylase 1 (LSD1) and histone deacetylases mediates antineoplastic efficacy of HDAC inhibitors in human breast cancer cells

(2013) Shauna N. Vasilatos et al.   CARCINOGENESIS

Identification of Small Molecule Inhibitors of Jumonji AT-rich Interactive Domain 1B (JARID1B) Histone Demethylase by a Sensitive High Throughput Screen

(2013) Joyce Sayegh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of the KDM2/7 Histone Lysine Demethylase Subfamily Inhibitor and its Antiproliferative Activity

(2013) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Triazole–Dithiocarbamate Based Selective Lysine Specific Demethylase 1 (LSD1) Inactivators Inhibit Gastric Cancer Cell Growth, Invasion, and Migration

(2013) Yi-Chao Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pan-Histone Demethylase Inhibitors Simultaneously Targeting Jumonji C and Lysine-Specific Demethylases Display High Anticancer Activities

(2013) Dante Rotili et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nonpeptidic Propargylamines as Inhibitors of Lysine Specific Demethylase 1 (LSD1) with Cellular Activity

(2013) Martin L. Schmitt et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-Throughput Virtual Screening Identifies Novel N′-(1-Phenylethylidene)-benzohydrazides as Potent, Specific, and Reversible LSD1 Inhibitors

(2013) Venkataswamy Sorna et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genome-wide localization of small molecules

(2013) Lars Anders et al.   NATURE BIOTECHNOLOGY

Histone lysine demethylases as targets for anticancer therapy

(2013) Jonas W. Højfeldt et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis and evaluation of 3-amino/guanidine substituted phenyl oxazoles as a novel class of LSD1 inhibitors with anti-proliferative properties

(2013) Balakrishna Dulla et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Targeting the JMJD2 Histone Demethylases to Epigenetically Control Herpesvirus Infection and Reactivation from Latency

(2013) Y. Liang et al.   Science Translational Medicine

5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation

(2013) Richard J. Hopkinson et al.   Chemical Science

Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments

(2013) James R. Hitchin et al.   MedChemComm

A Novel Selective LSD1/KDM1A Inhibitor Epigenetically Blocks Herpes Simplex Virus Lytic Replication and Reactivation from Latency

(2013) Y. Liang et al.   mBio

Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines

(2013) Sergiy Konovalov et al.   Journal of Ovarian Research

Lysine-Specific Histone Demethylase 1 Inhibitors Control Breast Cancer Proliferation in ERα-Dependent and -Independent Manners

(2012) Julie A. Pollock et al.   ACS Chemical Biology

Linking of 2-Oxoglutarate and Substrate Binding Sites Enables Potent and Highly Selective Inhibition of JmjC Histone Demethylases

(2012) Esther C. Y. Woon et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

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

Inhibiting Interactions of Lysine Demethylase LSD1 with Snail/Slug Blocks Cancer Cell Invasion

(2012) G. Ferrari-Amorotti et al.   CANCER RESEARCH

Studies of H3K4me3 demethylation by KDM5B/Jarid1B/PLU1 reveals strong substrate recognition in vitro and identifies 2,4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor

(2012) Line H. Kristensen et al.   FEBS Journal

Identification of catechols as histone-lysine demethylase inhibitors

(2012) Anders L. Nielsen et al.   FEBS LETTERS

Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor

(2012) Dominica Willmann et al.   INTERNATIONAL JOURNAL OF CANCER

Oncogenic features of the JMJD2A histone demethylase in breast cancer

(2012) WILLIAM L. BERRY et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases

(2012) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

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

Opening the door to an epigenetic target

(2012) Charlotte Harrison   NATURE REVIEWS DRUG DISCOVERY

Over-Expression of LSD1 Promotes Proliferation, Migration and Invasion in Non-Small Cell Lung Cancer

(2012) Tangfeng Lv et al.   PLoS One

Brain-Penetrant LSD1 Inhibitors Can Block Memory Consolidation

(2011) Ramesh Neelamegam et al.   ACS Chemical Neuroscience

Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors

(2011) Hanae Benelkebir et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inhibitors of histone demethylation and histone deacetylation cooperate in regulating gene expression and inhibiting growth in human breast cancer cells

(2011) Yi Huang et al.   BREAST CANCER RESEARCH AND TREATMENT

Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds

(2011) Kai-Hsuan Chang et al.   ChemMedChem

Lysine-specific demethylase 1 is highly expressed in solitary fibrous tumors, synovial sarcomas, rhabdomyosarcomas, desmoplastic small round cell tumors, and malignant peripheral nerve sheath tumors

(2011) Hans-Ulrich Schildhaus et al.   HUMAN PATHOLOGY

Cryptotanshinone down-regulates androgen receptor signaling by modulating lysine-specific demethylase 1 function

(2011) Ching-Yuan Wu et al.   INTERNATIONAL JOURNAL OF CANCER

Transcriptional regulation and multiple functions of MAO genes

(2011) Jean C. Shih et al.   JOURNAL OF NEURAL TRANSMISSION

A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases

(2011) Xuelai Luo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

JmjC-domain containing histone demethylase 1B-mediatedp15Ink4bsuppression promotes the proliferation of leukemic progenitor cells through modulation of cell cycle progression in acute myeloid leukemia

(2011) Satoki Nakamura et al.   MOLECULAR CARCINOGENESIS

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

Frequent mutations of chromatin remodeling genes in transitional cell carcinoma of the bladder

(2011) Yaoting Gui et al.   NATURE GENETICS

Inhibition of LSD1 sensitizes glioblastoma cells to histone deacetylase inhibitors

(2011) M. M. Singh et al.   NEURO-ONCOLOGY

Histone demethylase JMJD2B coordinates H3K4/H3K9 methylation and promotes hormonally responsive breast carcinogenesis

(2011) L. Shi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular Mimicry and Ligand Recognition in Binding and Catalysis by the Histone Demethylase LSD1-CoREST Complex

(2011) Riccardo Baron et al.   STRUCTURE

A Scaffold-Tree-Merging Strategy for Prospective Bioactivity Annotation of γ-Pyrones

(2010) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structurally Designedtrans-2-Phenylcyclopropylamine Derivatives Potently Inhibit Histone Demethylase LSD1/KDM1,,§

(2010) Shinya Mimasu et al.   BIOCHEMISTRY

Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor

(2010) Daisuke Ogasawara et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations

(2010) Sreenath V. Sharma et al.   CELL

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

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

Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

(2010) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, Enzyme-Inhibitory Activity, and Effect on Human Cancer Cells of a Novel Series of Jumonji Domain-Containing Protein 2 Histone Demethylase Inhibitors

(2010) Shohei Hamada et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule-Based Inhibition of Histone Demethylation in Cells Assessed by Quantitative Mass Spectrometry

(2010) Mukram M. Mackeen et al.   JOURNAL OF PROTEOME RESEARCH

Comparative Analysis of Small Molecules and Histone Substrate Analogues as LSD1 Lysine Demethylase Inhibitors

(2010) Jeffrey C. Culhane et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2

(2010) Claudia Binda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Human LSD2/KDM1b/AOF1 Regulates Gene Transcription by Modulating Intragenic H3K4me2 Methylation

(2010) Rui Fang et al.   MOLECULAR CELL

Lysine Methylation Regulates E2F1-Induced Cell Death

(2010) Haroula Kontaki et al.   MOLECULAR CELL

Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

(2010) Gillian L. Dalgliesh et al.   NATURE

Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates

(2010) Armin Thalhammer et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

(2010) Oliver N. F. King et al.   PLoS One

Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors

(2009) Shohei Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Glucocorticoid status affects antidepressant regulation of locus coeruleus tyrosine hydroxylase and dorsal raphé tryptophan hydroxylase gene expression

(2009) Willem Heydendael et al.   BRAIN RESEARCH

LSD1 Is a Subunit of the NuRD Complex and Targets the Metastasis Programs in Breast Cancer

(2009) Yan Wang et al.   CELL

Novel Oligoamine Analogues Inhibit Lysine-Specific Demethylase 1 and Induce Reexpression of Epigenetically Silenced Genes

(2009) Y. Huang et al.   CLINICAL CANCER RESEARCH

A Novel Mammalian Flavin-dependent Histone Demethylase

(2009) Aristotele Karytinos et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors

(2009) Rie Ueda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A miniaturized screen for inhibitors of Jumonji histone demethylases

(2009) Masaaki Sakurai et al.   Molecular BioSystems

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

(2009) Gijs van Haaften et al.   NATURE GENETICS

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

(2009) G Liu et al.   ONCOGENE

LSD1-mediated epigenetic modification is required for TAL1 function and hematopoiesis

(2009) X. Hu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Jmjd6 Catalyses Lysyl-Hydroxylation of U2AF65, a Protein Associated with RNA Splicing

(2009) Celia J. Webby et al.   SCIENCE

Epigenetic Multiple Ligands: Mixed Histone/Protein Methyltransferase, Acetyltransferase, and Class III Deacetylase (Sirtuin) Inhibitors

(2008) Antonello Mai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥

(2008) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

DNA Oxidation as Triggered by H3K9me2 Demethylation Drives Estrogen-Induced Gene Expression

(2008) B. Perillo et al.   SCIENCE