Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021

Synthesis of Carboxamide‐Containing Tranylcypromine Analogues as LSD1 (KDM1A) Inhibitors Targeting Acute Myeloid Leukemia

(2021) Maria Teresa Borrello et al.   ChemMedChem

Raloxifene, identified as a novel LSD1 inhibitor, suppresses the migration of renal cell carcinoma

(2021) Yuan Ma et al.   Future Medicinal Chemistry

Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1

(2021) Xing-Jie Dai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of KDM1A activity restores adult neurogenesis and improves hippocampal memory in a mouse model of Kabuki syndrome

(2021) Li Zhang et al.   Molecular Therapy-Methods & Clinical Development

LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models

(2021) Rina Baba et al.   Science Advances

Design, synthesis, and biological evaluation of 5‐aminotetrahydroquinoline‐based LSD1 inhibitors acting on Asp375

(2021) Jiangkun Yan et al.   ARCHIV DER PHARMAZIE

Discovery of higenamine as a potent, selective and cellular active natural LSD1 inhibitor for MLL-rearranged leukemia therapy

(2021) Yuan Fang et al.   BIOORGANIC CHEMISTRY

Safety, pharmacokinetics and pharmacodynamics of TAK‐418, a novel inhibitor of the epigenetic modulator lysine‐specific demethylase 1A

(2021) Wei Yin et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer

(2021) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Identification of Potent Lysine-Specific Demethylase 1 Inhibitor Peptides and Temporary Cyclization to Enhance Proteolytic Stability and Cell Growth-Inhibitory Activity

(2021) Hiroki Kitagawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of (2-Aminocyclopropyl)phenyl Derivatives as Novel Positron Emission Tomography Imaging Agents for Lysine-Specific Demethylase 1 in the Brain

(2021) Yasushi Hattori et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors

(2021) Ming-Jie Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors

(2021) Xiangyu Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and identification of two novel resveratrol derivatives as potential LSD1 inhibitors

(2021) Yongtao Xu et al.   Future Medicinal Chemistry

Discovery of quinazoline derivatives as a novel class of potent and in vivo efficacious LSD1 inhibitors by drug repurposing

(2021) Zhonghua Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Natural products as LSD1 inhibitors for cancer therapy

(2020) Yuan Fang et al.   Acta Pharmaceutica Sinica B

Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective

(2020) Xing-Jie Dai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of fenoldopam as a novel LSD1 inhibitor to abrogate the proliferation of renal cell carcinoma using drug repurposing strategy

(2020) Yan Zheng et al.   BIOORGANIC CHEMISTRY

Arborinine, a potential LSD1 inhibitor, inhibits epithelial-mesenchymal transition of SGC-7901 cells and adriamycin-resistant gastric cancer SGC-7901/ADR cells

(2020) Yafei Chu et al.   INVESTIGATIONAL NEW DRUGS

Discovery of orally active chalcones as histone lysine specific demethylase 1 inhibitors for the treatment of leukaemia

(2020) Yang Li et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma

(2020) M Naveen Sadhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Expanding the Role of the Histone Lysine-Specific Demethylase LSD1 in Cancer

(2019) Barbara Majello et al.   Cancers

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

(2019) Yuan Fang et al.   Journal of Hematology & Oncology

Anticancer activity of arborinine from Glycosmis parva leaf extract in human cervical cancer cells

(2018) Kitiya Piboonprai et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

(2018) Jay H. Kalin et al.   Nature Communications

Pharmacological Inhibition of LSD1 for Cancer Treatment

(2018) Guan-Jun Yang et al.   MOLECULES

T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice

(2018) Satoru Matsuda et al.   NEUROPSYCHOPHARMACOLOGY

Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment

(2017) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Applications of Higenamine in pharmacology and medicine

(2017) Nana Zhang et al.   JOURNAL OF ETHNOPHARMACOLOGY

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration

(2017) Luca Sartori et al.   JOURNAL OF MEDICINAL CHEMISTRY

Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells

(2017) Tinka Haydn et al.   Cell Death & Disease

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

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

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

(2015) Jianxun Wang et al.   NATURE NEUROSCIENCE

Medicinal chemistry insights in the discovery of novel LSD1 inhibitors

(2015) Xueshun Wang et al.   Epigenomics

Histone H3 lysine methylation in cognition and intellectual disability disorders

(2013) S. Parkel et al.   LEARNING & MEMORY

Perspectives on natural product epigenetic modulators in chemical biology and medicine

(2013) Fanny L. Cherblanc et al.   NATURAL PRODUCT REPORTS

Targeting H3K4 trimethylation in Huntington disease

(2013) M. Vashishtha 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

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

(2008) B. Perillo et al.   SCIENCE