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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.

European Institute Of Oncology

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.

European Institute Of Oncology

Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation.

Xinxiang Medical University

Discovery of [1,2,3]Triazolo[4,5-

Key Laboratory Of Technology Of Drug Preparation (Zhengzhou University)

Activation of lysine-specific demethylase 1 inhibitor peptide by redox-controlled cleavage of a traceless linker.

Nagoya City University

Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.

Tu Dortmund University

Efficient synthesis of new antiproliferative steroidal hybrids using the molecular hybridization approach.

Zhengzhou University

Recent Progress in Histone Demethylase Inhibitors.

University Of Oxford

Cyclopropanamine Compounds and Use Thereof.

Temple University

Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators.

Kyoto Prefectural University Of Medicine

Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide.

Waseda University

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

Baylor College Of Medicine

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.

Shandong University

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

Sapienza University Of Rome

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.

Sapienza University Of Rome

Design, synthesis, and structure-activity relationship of novel LSD1 inhibitors based on pyrimidine-thiourea hybrids as potent, orally active antitumor agents.

Zhengzhou University

Histone H3 peptide based LSD1-selective inhibitors.

Waseda University

Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures.

John Hopkins University

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.

European Institute Of Oncology

Synthesis and evaluation of novel cyclic Peptide inhibitors of lysine-specific demethylase 1.

Medical University Of South Carolina

High-throughput virtual screening identifies novel N'-(1-phenylethylidene)-benzohydrazides as potent, specific, and reversible LSD1 inhibitors.

University Of Utah

Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.

Zhengzhou University

Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity.

University Of Freiburg

Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1.

Wayne State University

Oncoepigenomics: making histone lysine methylation count.

TBA

(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.

Wayne State University

Lysine demethylases inhibitors.

Kyoto Prefectural University Of Medicine

Inhibitors of histone demethylases.

University Of Copenhagen

Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.

University Of Southampton

Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor.

Nagoya City University

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.

Constellation Pharmaceuticals

4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors.

Liaocheng University

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

European Institute Of Oncology Irccs

New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.

Universidad San Pablo-Ceu

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

Sichuan University

Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors.

Zhengzhou University

Discovery and synthesis of novel indole derivatives-containing 3-methylenedihydrofuran-2(3H)-one as irreversible LSD1 inhibitors.

Zhengzhou University

Synthesis, structure-activity relationship studies and biological characterization of new [1,2,4]triazolo[1,5-a]pyrimidine-based LSD1/KDM1A inhibitors.

Zhengzhou University

Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.

Liaoning Shihua University

Identification of selective and reversible LSD1 inhibitors with anti-metastasis activity by high-throughput docking.

Taizhou People'S Hospital

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

Zhengzhou University

Inhibition of the FAD containing ER oxidoreductin 1 (Ero1) protein by EN-460 as a strategy for treatment of multiple myeloma.

West Virginia University

Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors.

Shenyang Pharmaceutical University

Flavone-based natural product agents as new lysine-specific demethylase 1 inhibitors exhibiting cytotoxicity against breast cancer cells in vitro.

China Pharmaceutical University

Design, synthesis and in vitro evaluation of stilbene derivatives as novel LSD1 inhibitors for AML therapy.

Xinxiang Medical University

Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors.

Celgene

3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors.

Medical University Of South Carolina

Polyamine-based small molecule epigenetic modulators.

Wayne State University

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Sapienza University Of Rome

Recent advances in the development of polyamine analogues as antitumor agents.

Johns Hopkins University

Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.

University Of Freiburg

Optimization of 5-arylidene barbiturates as potent, selective, reversible LSD1 inhibitors for the treatment of acute promyelocytic leukemia.

Fudan University

Structure-based design and discovery of potent and selective KDM5 inhibitors.

Celgene

Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors.

Alma Mater Studiorum-University Of Bologna

New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma and embryonic carcinoma cells.

University Of Nevada

Design, synthesis and evaluation of ?-turn mimetics as LSD1-selective inhibitors.

Kyoto Prefectural University Of Medicine

Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors.

Waseda University

Discovery of tranylcypromine analogs with an acylhydrazone substituent as LSD1 inactivators: Design, synthesis and their biological evaluation.

Zhengzhou University

Lysine-Specific Demethylase 1 (LSD1) Inhibitors as Potential Treatment for Different Types of Cancers.

Therachem Research Medilab (India)

Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors.

East China Normal University

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

Xinxiang Medical University

Development and evaluation of 4-(pyrrolidin-3-yl)benzonitrile derivatives as inhibitors of lysine specific demethylase 1.

University Of Manchester

Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.

Zhengzhou University

Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A).

University Of East Anglia

3D-QSAR (CoMFA, CoMSIA), molecular docking and molecular dynamics simulations study of 6-aryl-5-cyano-pyrimidine derivatives to explore the structure requirements of LSD1 inhibitors.

Zhengzhou University

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

Genentech

Development of 5-hydroxypyrazole derivatives as reversible inhibitors of lysine specific demethylase 1.

University Of Manchester

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

University Of Manchester

Development and crystallographic evaluation of histone H3 peptide with N-terminal serine substitution as a potent inhibitor of lysine-specific demethylase 1.

Nagoya City University

Synthesis and biological evaluation of novel N, N'-disubstituted urea and thiourea derivatives as potential anti-melanoma agents.

Nanjing University

Heme Proximal Hydrogen Bonding between His170 and Asp132 Plays an Essential Role in the Heme Degradation Reaction of HutZ from Vibrio cholerae.

Hokkaido University

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain.

Oncology Innovative Medicines Unit

Correlation of the apparent affinities and efficacies of gamma-aminobutyric acid(C) receptor agonists.

University Of Alabama At Birmingham

Characterization of the binding site for a novel class of noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonists.

Pfizer

Structural elements of the gamma-aminobutyric acid type A receptor conferring subtype selectivity for benzodiazepine site ligands.

SynthÉLabo

Identification of pharmacological chaperones for Gaucher disease and characterization of their effects on beta-glucocerebrosidase by hydrogen/deuterium exchange mass spectrometry.

Research Institute, Hospital For Sick Children

Characterization of the cloned human mu opioid receptor.

University Of Pennsylvania

Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.

Merck Sharp & Dohme Research Laboratories

Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors.

Japan Tobacco

A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists.

University Of Arizona Tucson

Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.

Gnf

Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity.

Karo Bio

Synthesis and aminoacyl-tRNA synthetase inhibitory activity of aspartyl adenylate analogs.

Crefsip

Acylguanidines as small-molecule beta-secretase inhibitors.

Wyeth Research

Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).

Universite De Montreal At Succursale Centre-Ville

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

Astex

Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group.

Tohoku College Of Pharmacy

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.

Merck Research Laboratories

6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

Glaxosmithkline

Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.

University Of Newcastle

Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.

Sugen

3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase.

University Of Auckland

Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.

Hebrew University Of Jerusalem

Direct Interaction of Chivosazole F with Actin Elicits Cell Responses Similar to Latrunculin A but Distinct from Chondramide.

Novartis Pharma

Structure of the BH3 domains from the p53-inducible BH3-only proteins Noxa and Puma in complex with Mcl-1.

University Of Otago

Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.

Eli Lilly