LSD1: biologic roles and therapeutic targeting

Lysine-Specific Demethylase 1A (KDM1A/LSD1): Product Recognition and Kinetic Analysis of Full-Length Histones

(2016) Jonathan M. Burg et al.   BIOCHEMISTRY

Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

(2016) John P. McGrath et al.   CANCER RESEARCH

The LSD1 inhibitor RN-1 induces fetal hemoglobin synthesis and reduces disease pathology in sickle cell mice

(2015) S. Cui et al.   BLOOD

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

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

Lysine Demethylase LSD1 Coordinates Glycolytic and Mitochondrial Metabolism in Hepatocellular Carcinoma Cells

(2015) A. Sakamoto et al.   CANCER RESEARCH

A Systematic Review of Histone Lysine-Specific Demethylase 1 and Its Inhibitors

(2015) Yi-Chao Zheng et al.   MEDICINAL RESEARCH REVIEWS

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

(2015) Benoit Laurent et al.   MOLECULAR CELL

GFI1 proteins orchestrate the emergence of haematopoietic stem cells through recruitment of LSD1

(2015) Roshana Thambyrajah et al.   NATURE CELL BIOLOGY

Functional annotation of native enhancers with a Cas9–histone demethylase fusion

(2015) Nicola A Kearns et al.   NATURE METHODS

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

(2015) Jianxun Wang et al.   NATURE NEUROSCIENCE

Preclinical activity of combined HDAC and KDM1A inhibition in glioblastoma

(2015) Melissa M. Singh et al.   NEURO-ONCOLOGY

HMG20A is required for SNAI1-mediated epithelial to mesenchymal transition

(2015) S Rivero et al.   ONCOGENE

LSD1/KDM1A promotes hematopoietic commitment of hemangioblasts through downregulation of Etv2

(2015) Miki Takeuchi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease

(2015) Tamara Maes et al.   Epigenomics

LSD1 is essential for oocyte meiotic progression by regulating CDC25B expression in mice

(2015) Jeesun Kim et al.   Nature Communications

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

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

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

Differential Properties of Transcriptional Complexes Formed by the CoREST Family

(2014) A. P. Barrios et al.   MOLECULAR AND CELLULAR BIOLOGY

Destabilizing LSD1 by Jade-2 Promotes Neurogenesis: An Antibraking System in Neural Development

(2014) Xiao Han et al.   MOLECULAR CELL

Phosphorylation of LSD1 by PKCα Is Crucial for Circadian Rhythmicity and Phase Resetting

(2014) Hye Jin Nam et al.   MOLECULAR CELL

Antagonistic actions of Rcor proteins regulate LSD1 activity and cellular differentiation

(2014) G. Upadhyay et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chromatin state dynamics during blood formation

(2014) D. Lara-Astiaso et al.   SCIENCE

Lysine-Specific Demethylase 1 Has Dual Functions as a Major Regulator of Androgen Receptor Transcriptional Activity

(2014) Changmeng Cai et al.   Cell Reports

Lsd1 Restricts the Number of Germline Stem Cells by Regulating Multiple Targets in Escort Cells

(2014) Susan Eliazer et al.   PLoS Genetics

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

Insm1 controls development of pituitary endocrine cells and requires a SNAG domain for function and for recruitment of histone-modifying factors

(2013) J. E. Welcker et al.   DEVELOPMENT

The histone demethylase LSD1/KDM1A promotes the DNA damage response

(2013) Nima Mosammaparast et al.   JOURNAL OF CELL BIOLOGY

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

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

Phosphorylation of neuronal Lysine-Specific Demethylase 1LSD1/KDM1A impairs transcriptional repression by regulating interaction with CoREST and histone deacetylases HDAC1/2

(2013) Emanuela Toffolo et al.   JOURNAL OF NEUROCHEMISTRY

Modification of Enhancer Chromatin: What, How, and Why?

(2013) Eliezer Calo et al.   MOLECULAR CELL

Locus-specific editing of histone modifications at endogenous enhancers

(2013) Eric M Mendenhall et al.   NATURE BIOTECHNOLOGY

Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin induction

(2013) Lihong Shi et al.   NATURE MEDICINE

Histone lysine demethylases as targets for anticancer therapy

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

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

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

Histone demethylase Lsd1 represses hematopoietic stem and progenitor cell signatures during blood cell maturation

(2013) Marc A Kerenyi et al.   eLife

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

LSD1 inhibition: a therapeutic strategy in cancer?

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

Low Molecular Weight Amidoximes that Act as Potent Inhibitors of Lysine-Specific Demethylase 1

(2012) Stuart Hazeldine et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lysine-specific demethylase 1 restricts hematopoietic progenitor proliferation and is essential for terminal differentiation

(2012) A Sprüssel et al.   LEUKEMIA

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

LSD1/CoREST is an allosteric nanoscale clamp regulated by H3-histone-tail molecular recognition

(2012) R. Baron et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

FAD-dependent lysine-specific demethylase-1 regulates cellular energy expenditure

(2012) Shinjiro Hino et al.   Nature Communications

Novel Histone Demethylase LSD1 Inhibitors Selectively Target Cancer Cells with Pluripotent Stem Cell Properties

(2011) J. Wang et al.   CANCER RESEARCH

CoREST/LSD1 Control the Development of Pyramidal Cortical Neurons

(2011) Patricio Fuentes et al.   CEREBRAL CORTEX

Pioneer transcription factors: establishing competence for gene expression

(2011) K. S. Zaret et al.   GENES & DEVELOPMENT

Endogenous retroviruses and neighboring genes are coordinately repressed by LSD1/KDM1A

(2011) Todd S. Macfarlan et al.   GENES & DEVELOPMENT

LSD1 regulates the balance between self-renewal and differentiation in human embryonic stem cells

(2011) Antonio Adamo et al.   NATURE CELL BIOLOGY

miR-137 forms a regulatory loop with nuclear receptor TLX and LSD1 in neural stem cells

(2011) GuoQiang Sun et al.   Nature Communications

The SNAG domain of Snail1 functions as a molecular hook for recruiting lysine-specific demethylase 1

(2010) Yiwei Lin et al.   EMBO JOURNAL

Alternative Splicing of the Histone Demethylase LSD1/KDM1 Contributes to the Modulation of Neurite Morphogenesis in the Mammalian Nervous System

(2010) C. Zibetti et al.   JOURNAL OF NEUROSCIENCE

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

Histone Demethylase LSD1 Regulates Neural Stem Cell Proliferation

(2010) G. Sun et al.   MOLECULAR AND CELLULAR BIOLOGY

Lysine-Specific Demethylase 1 Regulates the Embryonic Transcriptome and CoREST Stability

(2010) C. T. Foster et al.   MOLECULAR AND CELLULAR BIOLOGY

Lysine Methylation Regulates E2F1-Induced Cell Death

(2010) Haroula Kontaki et al.   MOLECULAR CELL

Requirement of the histone demethylase LSD1 in Snai1-mediated transcriptional repression during epithelial-mesenchymal transition

(2010) T Lin et al.   ONCOGENE

Long Noncoding RNA as Modular Scaffold of Histone Modification Complexes

(2010) M.-C. Tsai et al.   SCIENCE

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

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

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

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

Direct Binding of CoREST1 to SUMO-2/3 Contributes to Gene-Specific Repression by the LSD1/CoREST1/HDAC Complex

(2009) Jian Ouyang et al.   MOLECULAR CELL

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

(2009) Yu Liang et al.   NATURE MEDICINE

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

The lysine demethylase LSD1 (KDM1) is required for maintenance of global DNA methylation

(2008) Jing Wang et al.   NATURE GENETICS