TCPs: privileged scaffolds for identifying potent LSD1 inhibitors for cancer therapy

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

Advances in the development of histone lysine demethylase inhibitors

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

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

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

RN-1, a potent and selective lysine-specific demethylase 1 inhibitor, increases γ-globin expression, F reticulocytes, and F cells in a sickle cell disease mouse model

(2015) Angela Rivers et al.   EXPERIMENTAL HEMATOLOGY

Overexpression of Lysine-Specific Demethylase 1 Is Associated With Tumor Progression and Unfavorable Prognosis in Chinese Patients With Endometrioid Endometrial Adenocarcinoma

(2015) Yun-Duo Liu et al.   INTERNATIONAL JOURNAL OF GYNECOLOGICAL CANCER

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

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

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

High-throughput screening to identify inhibitors of lysine demethylases

(2015) Molly Gale et al.   Epigenomics

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

(2015) Tamara Maes et al.   Epigenomics

Expression of Lysine-specific demethylase 1 in human epithelial ovarian cancer

(2015) Cong Chen et al.   Journal of Ovarian Research

LSD1 Overexpression Is Associated with Poor Prognosis in Basal-Like Breast Cancer, and Sensitivity to PARP Inhibition

(2015) Satoi Nagasawa et al.   PLoS One

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

High nuclear expression levels of histone-modifying enzymes LSD1, HDAC2 and SIRT1 in tumor cells correlate with decreased survival and increased relapse in breast cancer patients

(2014) Remco S Derr et al.   BMC CANCER

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

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

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

High expression of the histone demethylase LSD1 associates with cancer cell proliferation and unfavorable prognosis in tongue cancer

(2014) Chunping Yuan et al.   JOURNAL OF ORAL PATHOLOGY & MEDICINE

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

(2014) W Fiskus et al.   LEUKEMIA

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

LSD1 controls metastasis of androgen-independent prostate cancer cells through PXN and LPAR6

(2014) A Ketscher et al.   Oncogenesis

SYNTHESIS, LSD1 INHIBITORY ACTIVITY, AND LSD1 BINDING MODEL OF OPTICALLY PURE LYSINE-PCPA CONJUGATES

(2014) Yukihiro Itoh et al.   Computational and Structural Biotechnology Journal

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

(2013) J Ding et al.   BRITISH 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

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

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

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

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

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

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

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

(2012) Tangfeng Lv et al.   PLoS One

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

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 demethylases

(2011) Brian Lohse et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

Lysine Demethylases Inhibitors

(2011) Takayoshi Suzuki 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

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

PELP1 is a reader of histone H3 methylation that facilitates oestrogen receptor-α target gene activation by regulating lysine demethylase 1 specificity

(2010) Sujit S Nair et al.   EMBO REPORTS

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 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 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

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

Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25Å

(2007) Shinya Mimasu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS