Intermolecular insights into allosteric inhibition of histone lysine-specific demethylase 1

Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models

(2020) Alessia Romussi et al.   ACS Medicinal Chemistry Letters

Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification

(2020) Ying Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antiviral Properties of the LSD1 Inhibitor SP-2509

(2020) Mitchell R. Harancher et al.   JOURNAL OF VIROLOGY

The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer

(2020) Raffaella Soldi et al.   PLoS One

Synthesis, characterization, crystal structures, Hirshfeld surface analysis and DFT computational studies of new Schiff Bases derived from Phenylhydrazine

(2020) Sakineh Parvarinezhad et al.   JOURNAL OF MOLECULAR STRUCTURE

Epigenetic drugs and their molecular targets in testicular germ cell tumours

(2019) Sina Jostes et al.   Nature Reviews Urology

ZY0511, a novel, potent and selective LSD1 inhibitor, exhibits anticancer activity against solid tumors via the DDIT4/mTOR pathway

(2019) Yan Li et al.   CANCER LETTERS

Pre-clinical activity of combined LSD1 and mTORC1 inhibition in MLL-translocated acute myeloid leukaemia

(2019) Gauri Deb et al.   LEUKEMIA

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

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

Crystal Structure of LSD1 in Complex with 4-[5-(Piperidin-4-ylmethoxy)-2-(p-tolyl)pyridin-3-yl]benzonitrile

(2018) Hideaki Niwa et al.   MOLECULES

LSD1 activates a lethal prostate cancer gene network independently of its demethylase function

(2018) Archana Sehrawat et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lysine-Specific Demethylase 1A as a Promising Target in Acute Myeloid Leukemia

(2018) Daniela Magliulo et al.   Frontiers in Oncology

Ligand-based design, synthesis and biological evaluation of xanthine derivatives as LSD1/KDM1A inhibitors

(2018) Qi-Sheng Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure–Activity Relationship

(2017) Paola Vianello et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1

(2017) Daniel P. Mould et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen

(2016) Yosuke Ota et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Quantitative relationships between structure and cytotoxic activity of flavonoid derivatives. An application of Hirshfeld surface derived descriptors

(2016) Bogumiła Kupcewicz et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of novel ( E )- N ′-(2,3-dihydro-1 H -inden-1-ylidene) benzohydrazides as potent LSD1 inhibitors

(2016) Yang Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

LSD1 inhibitors: a patent review (2010-2015)

(2016) Giulia Stazi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

CHARMM36m: an improved force field for folded and intrinsically disordered proteins

(2016) Jing Huang et al.   NATURE METHODS

Relationship between LSD1 expression and E-cadherin expression in prostate cancer

(2015) Min Wang et al.   INTERNATIONAL UROLOGY AND NEPHROLOGY

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

(2015) Fangrui Wu 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 Systematic Review of Histone Lysine-Specific Demethylase 1 and Its Inhibitors

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

Computational Insight into p21-Activated Kinase 4 Inhibition: A Combined Ligand- and Structure-Based Approach

(2014) Rui-Juan Li et al.   ChemMedChem

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

(2014) W Fiskus et al.   LEUKEMIA

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

Performance of M06, M06-2X, and M06-HF Density Functionals for Conformationally Flexible Anionic Clusters: M06 Functionals Perform Better than B3LYP for a Model System with Dispersion and Ionic Hydrogen-Bonding Interactions

(2013) Martin Walker et al.   JOURNAL OF PHYSICAL CHEMISTRY A

LSD1/CoREST Reversible Opening–Closing Dynamics: Discovery of a Nanoscale Clamp for Chromatin and Protein Binding

(2012) Riccardo Baron et al.   BIOCHEMISTRY

Oncoepigenomics: Making histone lysine methylation count

(2012) Daniel DeCarlo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Triptolide induces cell-cycle arrest and apoptosis of human multiple myeloma cells in vitro via altering expression of histone demethylase LSD1 and JMJD2B

(2011) Lu Wen et al.   ACTA PHARMACOLOGICA SINICA

Lysine Demethylases Inhibitors

(2011) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prediction of Absolute Solvation Free Energies using Molecular Dynamics Free Energy Perturbation and the OPLS Force Field

(2010) Devleena Shivakumar et al.   Journal of Chemical Theory and Computation