175 articles for thisTarget
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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
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
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
(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.
Wayne State University
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
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Shanghai Institute of Materia Medica
-Methylpropargylamine-Conjugated Hydroxamic Acids as Dual Inhibitors of Monoamine Oxidase A and Histone Deacetylase for Glioma Treatment.
University of Southern California
Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles.
Riken Center For Sustainable Resource Science
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
Kyoto Prefectural University of Medicine
Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
Hangzhou Normal University
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
National Institute of Pharmaceutical Education and Research (NIPER)
A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.
Zhengzhou University
Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease.
Pharmaxis
Structure-Based Identification of Potent Lysine-Specific Demethylase 1 Inhibitor Peptides and Temporary Cyclization to Enhance Proteolytic Stability and Cell Growth-Inhibitory Activity.
Nagoya City University
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
Xinxiang Medical University
Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.
China Pharmaceutical University
Discovery of quinazoline derivatives as a novel class of potent and in vivo efficacious LSD1 inhibitors by drug repurposing.
Henan University of Chinese Medicine
Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.
Shenyang Pharmaceutical University
Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.
Zhengzhou University
Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective.
Key Laboratory of Henan Provinc
Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor ? (ER?) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer.
Wuhan University
Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma.
Jubilant Therapeutics India
[1,2,3]Triazolo[4,5-d]pyrimidine derivatives incorporating (thio)urea moiety as a novel scaffold for LSD1 inhibitors.
Henan University of Chinese Medicine
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
Fount Therapeutics
Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors.
Shenyang Pharmaceutical 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
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
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
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
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