201 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
Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region.
Shenzhen University
Design, synthesis and biological evaluation of nitric oxide-releasing 5-cyano-6-phenyl-2, 4-disubstituted pyrimidine derivatives.
Zhengzhou University
Design, synthesis and in vitro/in vivo anticancer activity of tranylcypromine-based triazolopyrimidine analogs as novel LSD1 inhibitors.
Henan University of Chinese Medicine
Identification of novel indole derivatives as highly potent and efficacious LSD1 inhibitors.
Shenyang Pharmaceutical University
Discovery of novel N-benzylarylamide-dithiocarbamate based derivatives as dual inhibitors of tubulin polymerization and LSD1 that inhibit gastric cancers.
Zhengzhou University
Discovery of acridine-based LSD1 inhibitors as immune activators targeting LSD1 in gastric cancer.
Zhengzhou University
Discovery of novel tranylcypromine-based derivatives as LSD1 inhibitors for gastric cancer treatment.
Zhengzhou University
Triazole-fused pyrimidines in target-based anticancer drug discovery.
Zhenzhou University
Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications.
Zhengzhou University
Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Takeda Pharmaceutical
Research progress of LSD1-based dual-target agents for cancer therapy.
Xinxiang University
Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors.
Xinxiang Medical University
Structural and Functional Landscape of FAD-Dependent Histone Lysine Demethylases for New Drug Discovery.
Zhengzhou University
Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells.
Zhengzhou University
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma.
Medical University of South Carolina
Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.
Hunan University of Science and Technology
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD).
University of S£O Paulo
Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1.
Zhengzhou University
Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021.
Zhengzhou 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 α (ERα) 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 γ-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
SUBSTITUTED N-CYANOPYRROLIDINES WITH ACTIVITY AS USP30 INHIBITORS
Mission Therapeutics
Vesicular monoamine transporter-2 ligands and their use in the treatment of psychostimulant abuse
University Of Kentucky Research Foundation
MODIFIED BENZOFURAN-CARBOXAMIDES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
Merck Sharp & Dohme
Bi-heteroaryl substitute 1,4-benzodiazepines and uses thereof for the treatment of cancer
Janssen Pharmaceutica
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
Beijing Tide Pharmaceutical
Substituted n-pyrimidin-4-yl-3-amino-pyrrolo[3,4-c]pyrazoles as protein kinase C inhibitors
Pfizer
3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
Board of Trustees of The Southern Illinois University
Substituted isoindolin-1-ones and 2,3-dihydro-1H-pyrrol[3,4-c]pyridin-1-ones as HPK1 antagonists
Nimbus Saturn
Type of aryl benzofuran amidated derivative and medical use thereof
China Pharmaceutical University
Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
Legochem Biosciences
(S)-2-(1-cyclopropylethyl)-5-(4-methyl-2-((6-(2-oxopyrrolidin-1-yl)pyridin-2-yl)amino) thiazol-5-yl)-7-(methylsulfonyl)isoindolin-1-one as a phosphatidylinositol 3-kinase inhibitor
Astrazeneca
Cyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide
Boehringer Ingelheim International
5-[3-[piperazin-1-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS 4 and 5 inhibitors for treating e.g. osteoarthritis
Galapagos
Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
Allergan
Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
Forma Therapeutics
Compositions and methods for treating neoplasia, inflammatory disease and other disorders
Dana-Farber Cancer Institute
Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
Bristol-Myers Squibb
Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments
Bayer Intellectual Property
Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
Euroscreen
Substituted azoles, antiviral active component, pharmaceutical composition, method for preparation and use thereof
TBA
Designing modulators of dimethylarginine dimethylaminohydrolase (DDAH): a focus on selectivity over arginase.
Christian-Albrechts-University
Synthesis of 5-amino-1,3,4-thiadiazole-2-sulphonamide derivatives and their inhibition effects on human carbonic anhydrase isozymes.
Dumlupinar University
Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine.
Academy of Sciences of The Czech Republic
Rationalizing the Binding Kinetics for the Inhibition of the Burkholderia pseudomallei FabI1 Enoyl-ACP Reductase.
Stony Brook University
Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.
The University of Sydney
A L-lysine transporter of high stereoselectivity of the amino acid-polyamine-organocation (APC) superfamily: production, functional characterization, and structure modeling.
Max Planck Institute of Biophysics
Some Anticancer Agents Act on Human Serum Paraoxonase-1 to Reduce Its Activity.
Ahi Evran University
2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-YL)picolinamide derivatives as orexin receptor antagonists
Actelion Pharmaceuticals
Tri-aryl/heteroaromatic cannabinoids and use thereof
The University of Tennessee Research Foundation
Azetidine derivative and antidepressant composition including the same
Korea Institute of Science and Technology
Enzymatic Studies of Isoflavonoids as Selective and Potent Inhibitors of Human Leukocyte 5-Lipo-Oxygenase.
Universidad De Santiago
1,2-Diaryl-2-hydroxyiminoethanones as dual COX-1 and ß-amyloid aggregation inhibitors: biological evaluation and in silico study.
Mazandaran University of Medical Sciences
Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
University of South Florida
Structure-based design of potent small-molecule binders to the S-component of the ECF transporter for thiamine.
University of Groningen
Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
Vitae Pharmaceuticals
Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.
University of Toronto
Structure-aided optimization of kinase inhibitors derived from alsterpaullone.
Technische UniversitÄT Braunschweig