A Systematic Review of Histone Lysine-Specific Demethylase 1 and Its Inhibitors
Published 2015 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
A Systematic Review of Histone Lysine-Specific Demethylase 1 and Its Inhibitors
Authors
Keywords
-
Journal
MEDICINAL RESEARCH REVIEWS
Volume 35, Issue 5, Pages 1032-1071
Publisher
Wiley
Online
2015-05-19
DOI
10.1002/med.21350
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A
- (2015) Marco Pieroni et al. EUROPEAN 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
- RNA epigenetics
- (2015) Nian Liu et al. Translational Research
- 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
- Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells
- (2015) Veronica Rodriguez et al. MedChemComm
- A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1
- (2014) Polina Prusevich et al. ACS Chemical Biology
- Inhibition of lysine-specific demethylase 1 by the acyclic diterpenoid geranylgeranoic acid and its derivatives
- (2014) Chiharu Sakane et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Sensing core histone phosphorylation — A matter of perfect timing
- (2014) Anna Sawicka et al. Biochimica et Biophysica Acta-Gene Regulatory Mechanisms
- Targeting histone lysine demethylases — Progress, challenges, and the future
- (2014) Cyrille C. Thinnes et al. Biochimica et Biophysica Acta-Gene Regulatory Mechanisms
- Reversing DNA Methylation: Mechanisms, Genomics, and Biological Functions
- (2014) Hao Wu et al. CELL
- 212 Novel anti-tumor activity of targeted LSD1 inhibition by GSK2879552
- (2014) H. Mohammad et al. EUROPEAN JOURNAL OF CANCER
- Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: A novel class of irreversible inhibitors of histone demethylase KDM1A
- (2014) Paola Vianello et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Loss of 5-hydroxymethylcytosine in cancer: Cause or consequence?
- (2014) Gabriella Ficz et al. GENOMICS
- DNA demethylation, Tet proteins and 5-hydroxymethylcytosine in epigenetic reprogramming: An emerging complex story
- (2014) Peter W.S. Hill et al. GENOMICS
- Identification of Myelin Transcription Factor 1 (MyT1) as a Subunit of the Neural Cell Type-specific Lysine-specific Demethylase 1 (LSD1) Complex
- (2014) Atsushi Yokoyama et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells
- (2014) W Fiskus et al. LEUKEMIA
- Reversible Inhibitors of LSD1 as Therapeutic Agents in Acute Myeloid Leukemia: Clinical Significance and Progress to Date
- (2014) Daniel P. Mould et al. MEDICINAL RESEARCH REVIEWS
- Destabilizing LSD1 by Jade-2 Promotes Neurogenesis: An Antibraking System in Neural Development
- (2014) Xiao Han et al. MOLECULAR CELL
- Synthesis and biological evaluation of coumarin–1,2,3-triazole–dithiocarbamate hybrids as potent LSD1 inhibitors
- (2014) Xian-Wei Ye 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
- Lysine-specific demethylase 1 regulates differentiation onset and migration of trophoblast stem cells
- (2014) Dongmei Zhu et al. Nature Communications
- LSD1 promotes oxidative metabolism of white adipose tissue
- (2014) Delphine Duteil et al. Nature Communications
- TERRA-Reinforced Association of LSD1 with MRE11 Promotes Processing of Uncapped Telomeres
- (2014) Antonio Porro et al. Cell Reports
- 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
- LSD1-mediated epigenetic modification contributes to proliferation and metastasis of colon cancer
- (2013) J Ding et al. BRITISH JOURNAL OF CANCER
- miR-329 suppresses the growth and motility of neuroblastoma by targeting KDM1A
- (2013) Haifeng Yang et al. FEBS LETTERS
- MiR-137 functions as a tumor suppressor in neuroblastoma by downregulating KDM1A
- (2013) Kristina Althoff et al. INTERNATIONAL JOURNAL OF CANCER
- 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
- Concerted Hydrogen Atom and Electron Transfer Mechanism for Catalysis by Lysine-Specific Demethylase
- (2013) Tao Yu et al. JOURNAL OF PHYSICAL CHEMISTRY B
- 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
- Prox1 Directly Interacts with LSD1 and Recruits the LSD1/NuRD Complex to Epigenetically Co-Repress CYP7A1 Transcription
- (2013) Huafang Ouyang et al. PLoS One
- Lysine-Specific Demethylase 1 (LSD1/KDM1A) Contributes to Colorectal Tumorigenesis via Activation of the Wnt/Β-Catenin Pathway by Down-Regulating Dickkopf-1 (DKK1)
- (2013) Zebin Huang et al. PLoS One
- The Role of the CoREST/REST Repressor Complex in Herpes Simplex Virus 1 Productive Infection and in Latency
- (2013) Guoying Zhou et al. Viruses-Basel
- Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
- (2013) James R. Hitchin et al. MedChemComm
- Synthesis and Evaluation of Novel Cyclic Peptide Inhibitors of Lysine-Specific Demethylase 1
- (2013) Isuru R. Kumarasinghe et al. ACS Medicinal Chemistry Letters
- Molecular dynamics simulations indicate an induced-fit mechanism for LSD1/CoREST-H3-histone molecular recognition
- (2013) Nadeem A Vellore et al. BMC Biophysics
- Pluripotent Stem Cell Protein Sox2 Confers Sensitivity to LSD1 Inhibition in Cancer Cells
- (2013) Xiaoming Zhang et al. Cell Reports
- The Deubiquitinase USP28 Stabilizes LSD1 and Confers Stem-Cell-like Traits to Breast Cancer Cells
- (2013) Yadi Wu et al. Cell Reports
- Expanding the Druggable Space of the LSD1/CoREST Epigenetic Target: New Potential Binding Regions for Drug-Like Molecules, Peptides, Protein Partners, and Chromatin
- (2013) James C. Robertson et al. PLoS Computational Biology
- Histone demethylase Lsd1 represses hematopoietic stem and progenitor cell signatures during blood cell maturation
- (2013) Marc A Kerenyi et al. eLife
- 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
- The histone demethylase LSD1 is required for estrogen-dependent S100A7 gene expression in human breast cancer cells
- (2012) Seung Eun Yu et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Loss of LSD1 (lysine-specific demethylase 1) suppresses growth and alters gene expression of human colon cancer cells in a p53- and DNMT1(DNA methyltransferase 1)-independent manner
- (2012) Lihua Jin et al. BIOCHEMICAL JOURNAL
- LSD1/CoREST Reversible Opening–Closing Dynamics: Discovery of a Nanoscale Clamp for Chromatin and Protein Binding
- (2012) Riccardo Baron et al. BIOCHEMISTRY
- Breaking the LSD1/KDM1A Addiction: Therapeutic Targeting of the Epigenetic Modifier in AML
- (2012) Alyson A. Lokken et al. CANCER CELL
- 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
- Mechanisms of human histone and nucleic acid demethylases
- (2012) Louise J Walport et al. CURRENT OPINION IN CHEMICAL BIOLOGY
- LSD1 inhibition: a therapeutic strategy in cancer?
- (2012) James T Lynch et al. EXPERT OPINION ON THERAPEUTIC TARGETS
- Negative regulation of ERα by a novel protein CAC1 through association with histone demethylase LSD1
- (2012) JuHyun Kim et al. FEBS LETTERS
- Lysine-specific demethylase 1 (LSD1/KDM1A/AOF2/BHC110) is expressed and is an epigenetic drug target in chondrosarcoma, Ewing's sarcoma, osteosarcoma, and rhabdomyosarcoma
- (2012) Idriss M. Bennani-Baiti et al. HUMAN PATHOLOGY
- 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
- Low Molecular Weight Amidoximes that Act as Potent Inhibitors of Lysine-Specific Demethylase 1
- (2012) Stuart Hazeldine et al. JOURNAL OF MEDICINAL CHEMISTRY
- LSD2/KDM1B and Its Cofactor NPAC/GLYR1 Endow a Structural and Molecular Model for Regulation of H3K4 Demethylation
- (2012) Rui Fang et al. MOLECULAR CELL
- 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
- Over-Expression of LSD1 Promotes Proliferation, Migration and Invasion in Non-Small Cell Lung Cancer
- (2012) Tangfeng Lv et al. PLoS One
- Reversible RNA adenosine methylation in biological regulation
- (2012) Guifang Jia et al. TRENDS IN GENETICS
- FAD-dependent lysine-specific demethylase-1 regulates cellular energy expenditure
- (2012) Shinjiro Hino et al. Nature Communications
- Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors
- (2011) Hanae Benelkebir et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Inhibitors of histone demethylases
- (2011) Brian Lohse 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
- Androgen Receptor Gene Expression in Prostate Cancer Is Directly Suppressed by the Androgen Receptor Through Recruitment of Lysine-Specific Demethylase 1
- (2011) Changmeng Cai et al. CANCER CELL
- Abnormal Histone Acetylation and Methylation Levels in Esophageal Squamous Cell Carcinomas
- (2011) Chen Chen et al. CANCER INVESTIGATION
- Inhibition of Histone Lysine Methylation Enhances Cancer-Testis Antigen Expression in Lung Cancer Cells: Implications for Adoptive Immunotherapy of Cancer
- (2011) M. Rao et al. CANCER RESEARCH
- Binding of the JmjC Demethylase JARID1B to LSD1/NuRD Suppresses Angiogenesis and Metastasis in Breast Cancer Cells by Repressing Chemokine CCL14
- (2011) Q. Li et al. CANCER RESEARCH
- Novel Histone Demethylase LSD1 Inhibitors Selectively Target Cancer Cells with Pluripotent Stem Cell Properties
- (2011) J. Wang et al. CANCER RESEARCH
- LSD1 and pluripotency: A new player in the network
- (2011) Antonio Adamo et al. CELL CYCLE
- Lysine Demethylases Inhibitors
- (2011) Takayoshi Suzuki et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Checkpoints of Viral Gene Expression in Productive and Latent Infection: the Role of the HDAC/CoREST/LSD1/REST Repressor Complex
- (2011) B. Roizman JOURNAL OF VIROLOGY
- 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
- A SIRT1-LSD1 Corepressor Complex Regulates Notch Target Gene Expression and Development
- (2011) Peter Mulligan et al. MOLECULAR CELL
- N6-Methyladenosine in nuclear RNA is a major substrate of the obesity-associated FTO
- (2011) Guifang Jia et al. Nature Chemical Biology
- LSD1 cooperates with CTIP2 to promote HIV-1 transcriptional silencing
- (2011) V. Le Douce et al. NUCLEIC ACIDS RESEARCH
- RCOR2 Is a Subunit of the LSD1 Complex That Regulates ESC Property and Substitutes for SOX2 in Reprogramming Somatic Cells to Pluripotency
- (2011) Peng Yang et al. STEM CELLS
- miR-137 forms a regulatory loop with nuclear receptor TLX and LSD1 in neural stem cells
- (2011) GuoQiang Sun et al. Nature Communications
- Embryonic stem cell-specific signatures in cancer: insights into genomic regulatory networks and implications for medicine
- (2011) Jonghwan Kim et al. Genome Medicine
- Activation of HIV Transcription by the Viral Tat Protein Requires a Demethylation Step Mediated by Lysine-specific Demethylase 1 (LSD1/KDM1)
- (2011) Naoki Sakane et al. PLoS Pathogens
- Reversal of Histone Methylation: Biochemical and Molecular Mechanisms of Histone Demethylases
- (2010) Nima Mosammaparast et al. Annual Review of Biochemistry
- Histone demethylase LSD1 is required to induce skeletal muscle differentiation by regulating myogenic factors
- (2010) Jinmi Choi et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Structurally Designedtrans-2-Phenylcyclopropylamine Derivatives Potently Inhibit Histone Demethylase LSD1/KDM1,,§
- (2010) Shinya Mimasu et al. BIOCHEMISTRY
- Demethylation of RB Regulator MYPT1 by Histone Demethylase LSD1 Promotes Cell Cycle Progression in Cancer Cells
- (2010) H.-S. Cho et al. CANCER RESEARCH
- AOF1 is a histone H3K4 demethylase possessing demethylase activity-independent repression function
- (2010) Ze Yang et al. CELL RESEARCH
- Structural insights into histone lysine demethylation
- (2010) Haifeng Hou et al. CURRENT OPINION IN STRUCTURAL BIOLOGY
- The SNAG domain of Snail1 functions as a molecular hook for recruiting lysine-specific demethylase 1
- (2010) Yiwei Lin et al. EMBO JOURNAL
- Overexpression of LSD1 contributes to human carcinogenesis through chromatin regulation in various cancers
- (2010) Shinya Hayami et al. INTERNATIONAL JOURNAL OF CANCER
- Histone Demethylase LSD1 Regulates Adipogenesis
- (2010) Melina M. Musri et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- (Bis)urea and (Bis)thiourea Inhibitors of Lysine-Specific Demethylase 1 as Epigenetic Modulators
- (2010) Shiv K. Sharma et al. JOURNAL OF MEDICINAL CHEMISTRY
- New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays
- (2010) Jonathan B. Baell et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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
- Lysine-Specific Demethylase 1 Regulates the Embryonic Transcriptome and CoREST Stability
- (2010) C. T. Foster et al. MOLECULAR AND CELLULAR BIOLOGY
- Human LSD2/KDM1b/AOF1 Regulates Gene Transcription by Modulating Intragenic H3K4me2 Methylation
- (2010) Rui Fang et al. MOLECULAR CELL
- A Feed-Forward Circuit Controlling Inducible NF-κB Target Gene Activation by Promoter Histone Demethylation
- (2010) Dominic van Essen et al. MOLECULAR CELL
- Lysine Methylation Regulates E2F1-Induced Cell Death
- (2010) Haroula Kontaki et al. MOLECULAR CELL
- Grand Challenge Commentary: RNA epigenetics?
- (2010) Chuan He Nature Chemical Biology
- Requirement of the histone demethylase LSD1 in Snai1-mediated transcriptional repression during epithelial-mesenchymal transition
- (2010) T Lin et al. ONCOGENE
- Disruption of HDAC/CoREST/REST repressor by dnREST reduces genome silencing and increases virulence of herpes simplex virus
- (2010) T. Du et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Chromatin Higher-order Structure and Dynamics
- (2010) C. L. Woodcock et al. Cold Spring Harbor Perspectives in Biology
- Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology
- (2009) Soyoung Lim et al. CARCINOGENESIS
- LSD1 Is a Subunit of the NuRD Complex and Targets the Metastasis Programs in Breast Cancer
- (2009) Yan Wang et al. CELL
- A C. elegans LSD1 Demethylase Contributes to Germline Immortality by Reprogramming Epigenetic Memory
- (2009) David J. Katz 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
- New roles of flavoproteins in molecular cell biology: Histone demethylase LSD1 and chromatin
- (2009) Federico Forneris et al. FEBS Journal
- ASXL1 Represses Retinoic Acid Receptor-mediated Transcription through Associating with HP1 and LSD1
- (2009) Sang-Wang Lee et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- 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
- Engagement of the Lysine-Specific Demethylase/HDAC1/CoREST/REST Complex by Herpes Simplex Virus 1
- (2009) H. Gu et al. JOURNAL OF VIROLOGY
- Involvement of Histone Demethylase LSD1 in Blimp-1-Mediated Gene Repression during Plasma Cell Differentiation
- (2009) S.-T. Su et al. MOLECULAR AND CELLULAR BIOLOGY
- KDM1B is a histone H3K4 demethylase required to establish maternal genomic imprints
- (2009) David N. Ciccone et al. NATURE
- Inhibition of the histone demethylase LSD1 blocks α-herpesvirus lytic replication and reactivation from latency
- (2009) Yu Liang et al. NATURE MEDICINE
- Histones: Annotating Chromatin
- (2008) Eric I. Campos et al. Annual Review of Genetics
- Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B
- (2008) David M. Gooden et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Connecting microRNA Genes to the Core Transcriptional Regulatory Circuitry of Embryonic Stem Cells
- (2008) Alexander Marson et al. CELL
- Integration of External Signaling Pathways with the Core Transcriptional Network in Embryonic Stem Cells
- (2008) Xi Chen et al. CELL
- An Extended Transcriptional Network for Pluripotency of Embryonic Stem Cells
- (2008) Jonghwan Kim et al. CELL
- Mechanisms involved in the regulation of histone lysine demethylases
- (2008) Fei Lan et al. CURRENT OPINION IN CELL BIOLOGY
- Cell Cycle Association of the Retinoblastoma Protein Rb and the Histone Demethylase LSD1 with the Epstein-Barr Virus Latency Promoter Cp
- (2008) C. M. Chau et al. JOURNAL OF VIROLOGY
- Histone Ubiquitination: Triggering Gene Activity
- (2008) Vikki M. Weake et al. MOLECULAR CELL
- The lysine demethylase LSD1 (KDM1) is required for maintenance of global DNA methylation
- (2008) Jing Wang et al. NATURE GENETICS
- Structure of human monoamine oxidase A at 2.2-A resolution: The control of opening the entry for substrates/inhibitors
- (2008) S.-Y. Son et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Add your recorded webinar
Do you already have a recorded webinar? Grow your audience and get more views by easily listing your recording on Peeref.
Upload NowCreate your own webinar
Interested in hosting your own webinar? Check the schedule and propose your idea to the Peeref Content Team.
Create Now