180 articles for L Wu
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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
Design, synthesis and biological evaluation of 3'-benzylated analogs of 3'-epi-neoponkoranol as potenta-glucosidase inhibitors.
China Pharmaceutical University
Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers.
University of Alabama At Birmingham
Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors.
Indiana University School of Medicine
A potent and selective inhibitor for the UBLCP1 proteasome phosphatase.
Indiana University
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Boehringer Ingelheim Pharmaceuticals
Selective CB2 receptor agonists. Part 1: the identification of novel ligands through computer-aided drug design (CADD) approaches.
Boehringer Ingelheim Pharmaceuticals
Synthesis and bioevaluation of 2-phenyl-4-methyl-1,3-selenazole-5-carboxylic acids as potent xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Therapeutic potential of targeting the oncogenic SHP2 phosphatase.
Indiana University School of Medicine
Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.
Boehringer Ingelheim Pharmaceuticals
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
Boehringer Ingelheim Pharma
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Tianjin University of Science and Technology
cis-1-Oxo-heterocyclyl-4-amido cyclohexane derivatives as NPY5 receptor antagonists.
Lundbeck Research Usa
A potent and selective small-molecule inhibitor for the lymphoid-specific tyrosine phosphatase (LYP), a target associated with autoimmune diseases.
Indiana University School of Medicine
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
Nankai University
Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors.
Peking Union Medical College
Discovery and evaluation of novel inhibitors of mycobacterium protein tyrosine phosphatase B from the 6-Hydroxy-benzofuran-5-carboxylic acid scaffold.
Indiana University School of Medicine
Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists.
Lundbeck Research Usa
Identification and characterization of novel inhibitors of mPTPB, an essential virulent phosphatase from Mycobacterium tuberculosis.
Indiana University School of Medicine
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215
Bristol-Myers Squibb Research and Development
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
Millennium Pharmaceuticals
Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.
Cv Therapeutics
Synthesis and characterization of a novel class of protein tyrosine phosphatase inhibitors.
New York University
N-Heteroaryl glycinamides and glycinamines as potent NPY5 antagonists.
Lundbeck Research Usa
Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters.
Boehringer Ingelheim Pharmaceuticals
Small molecule inhibitors of SHP2 tyrosine phosphatase discovered by virtual screening.
Indiana University
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.
Boehringer Ingelheim Pharmaceuticals
Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2).
Indiana University School of Medicine
Discovery of X10g as a selective PROTAC degrader of Hsp90α protein for treating breast cancer.
Fujian Medical University (FMU)
Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1H-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.
Shenyang Pharmaceutical University
Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer.
Jincheng People's Hospital
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
Incyte
Drug development and potential targets for Cushing's syndrome.
China Pharmaceutical University
The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.
China Pharmaceutical University
Discovery of potent and novel dual NAMPT/BRD4 inhibitors for efficient treatment of hepatocellular carcinoma.
Xinxiang Medical University
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer's disease.
Shenyang Pharmaceutical University
Discovery of Novel PTP1B Inhibitors with Once-Weekly Therapeutic Potential for Type 2 Diabetes: Design, Synthesis, and
Qingdao University
Design and Synthesis of Sulfonium Derivatives: A Novel Class of α-Glucosidase Inhibitors with Potent In Vivo Antihyperglycemic Activities.
China Pharmaceutical University
Structure-Based Design of Active-Site-Directed, Highly Potent, Selective, and Orally Bioavailable Low-Molecular-Weight Protein Tyrosine Phosphatase Inhibitors.
Eli Lilly
Recent advances in combretastatin A-4 codrugs for cancer therapy.
Xinxiang Medical University
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease.
Shenyang Pharmaceutical University
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.
Fujian Medical University (Fmu)
-Acylamino Saccharin as an Emerging Cysteine-Directed Covalent Warhead and Its Application in the Identification of Novel FBPase Inhibitors toward Glucose Reduction.
Central China Normal University
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.
Shenyang Pharmaceutical University
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.
Northwest University
Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.
University of Bras£Lia
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors.
Nih
Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Northwest University
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Incyte
Novel 5-fluorouracil sensitizers for colorectal cancer therapy: Design and synthesis of S1P receptor 2 (S1PR2) antagonists.
Ocean University of China
Exploration of 4-(1H-indol-3-yl)cyclohex-3-en-1-amine analogues as HDAC inhibitors: Design, synthesis, biological evaluation and modelling studies.
Shenyang Pharmaceutical University
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Astrazeneca
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).
Millennium Pharmaceuticals
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).
Cv Therapeutics
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Wake Forest University School of Medicine
Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration.
Nih
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Incyte
Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase.
National Cancer Institute-Frederick
Inhibition of Low Molecular Weight Protein Tyrosine Phosphatase by an Induced-Fit Mechanism.
Purdue University
Discovery of Novel PTP1B Inhibitors Derived from the BH3 Domain of Proapoptotic Bcl-2 Proteins with Antidiabetic Potency.
Qingdao University of Science and Technology
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357.
Boehringer Ingelheim Pharmaceuticals
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
Wake Forest University School of Medicine
Utilization of a peptide lead for the discovery of a novel PTP1B-binding motif.
National Cancer Institute-Frederick
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.
Fujian Medical University (Fmu)
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
Wake Forest University School of Medicine
Examination of novel non-phosphorus-containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains.
National Cancer Institute-Bethesda
PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b]naphtho[2,3-d]thiophenes.
Wyeth-Ayerst Research
BH3 mimetics derived from Bim-BH3 domain core region show PTP1B inhibitory activity.
Ocean University of China
Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT).
National Cancer Institute-Bethesda
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
Wake Forest University School of Medicine
Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis.
Indiana University School of Medicine
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.
University of Massachusetts-Boston
Discovery and optimization of oxadiazole-based FLAP inhibitors.
Boehringer Ingelheim Pharmaceuticals
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
The University of Texas M.D. Anderson Cancer Center
3-CYCLOAMINO-INDOLE COMPOUNDS AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Mindset Pharma
IMIDAZO[1,2-B]PYRIDAZINE BASED TRICYCLIC COMPOUNDS AS INHIBITORS OF HASPIN AND THERAPEUTIC USES THEREOF
CNIO
Vesicular monoamine transporter-2 ligands and their use in the treatment of psychostimulant abuse
University Of Kentucky Research Foundation
4-ALKOXYPYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF
Biosplice Therapeutics
Substituted pyrazolo[4,3-d]pyrimidines and imidazo[5,1 -f][1,2,4]triazines as androgen receptor and phosphodiesterase dual inhibitors
Ildong Pharmaceutical
Carboxylic acid, acyl sulfonamide and acyl sulfamide-derivatized bicyclic aza-heteroaromatics as selective Mcl-1 inhibitors and as dual Mcl-1/Bcl-2 inhibitors
University of Maryland, Baltimore
5-substituted difluoropiperidine compounds with blood-brain barrier penetrable capability
Wayshine Biopharm Holding
Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
Astrazeneca
Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
Hoffmann-La Roche
Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders
Mindset Pharma
Amide compounds as kinase inhibitors, compositions and methods of treatment
Translational Drug Development
Combination of pure 5-HT6 receptor antagonists with acetylcholinesterase inhibitors
Suven Life Sciences
Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors
Shenzhen Targetrx
Substituted 1,2,3,4-tetrahydroquinolines as inhibitors of repair enzyme 8-oxoguanine deoxyribonucleic acid glycosylase activity
The Leland Stanford Junior University
Bromodomain inhibitor compound and use thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
Beijing Tide Pharmaceutical
Identification of stabilizers of multimeric proteins
Leland Stanford Junior University
Imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase
University of Alberta
4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament
Boehringer Ingelheim International
Substituted imidazoles as apoptosis signal regulating kinase 1 inhibitors
Jiangsu Hansoh Pharmaceutical Group
4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament
Boehringer Ingelheim International
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Arena Pharmaceuticals
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors
Eli Lilly
Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
Legochem Biosciences
Quinoline and isoquinoline derivatives for treating pain and pain related conditions
Esteve Pharmaceuticals
Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
Allergan
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
Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.
Solapur University
Substituted azoles, antiviral active component, pharmaceutical composition, method for preparation and use thereof
TBA
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
Galderma Research & Devlopment
Delineation of the Pasteurellaceae-specific GbpA-family of glutathione-binding proteins.
Ghent University
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
Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase
Janssen Pharmaceutica
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
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
German Cancer Research Center (Dkfz)
Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor
Taiho Pharmaceutical
Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
University of South Florida
Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
Vitae Pharmaceuticals
Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.
Case Western Reserve University
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Pfizer
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Merck Frosst Canada