102 articles for J Lu
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Discovery of 4-((3'R,4'S,5'R)-6¿-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2¿-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3¿-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Deve
University of Michigan Comprehensive Cancer Center
Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.
College of Chemical and Environmental Engineering
Identification and in Vivo Evaluation of Liver X Receptorß-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Wuxi Apptec
Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.
Shanghai Jiao Tong University
Design of High-Affinity Stapled Peptides To Target the Repressor Activator Protein 1 (RAP1)/Telomeric Repeat-Binding Factor 2 (TRF2) Protein-Protein Interaction in the Shelterin Complex.
University of Michigan
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening.
Shanghai University
Chemical synthesis of tetracyclic terpenes and evaluation of antagonistic activity on endothelin-A receptors and voltage-gated calcium channels.
Kansas State University
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Merck Research Laboratories
Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3ß of substituted quinolines.
Kansas State University
Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles.
University of Michigan Comprehensive Cancer Center and Departments of Internal Medicine
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
Chinese Academy of Sciences
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
Merck Research Laboratories
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.
Chinese Academy of Sciences
Discovery of MK-7655, aß-lactamase inhibitor for combination with Primaxin®.
Merck Research Labs
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
University of Michigan
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.
Pfizer
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
University of Michigan
Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.
Duke University Medical Center
Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
University of Michigan
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
University of Michigan
Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.
Polaris Pharmaceuticals
Side chain SAR of bicyclicß-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.
Merck Research Labs
Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
University of Michigan
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
University of Michigan
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
Sun Yat-Sen University
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.
Merck Research Labs
Structure-activity relationship studies of small-molecule inhibitors of Wnt response.
The University of Texas Southwestern Medical Center At Dallas
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Pfizer
Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.
University of Michigan
Metabolism-guided development of Ko143 analogs as ABCG2 inhibitors.
University of Pittsburgh
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone.
Fudan University
Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors.
Yantai University
Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect.
Fudan University
Discovery and Evaluation of C6-Substituted Pyrazolopyrimidine-Based Bisphosphonate Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase and Evaluation of Their Antitumor Efficacy in Multiple Myeloma, Pancreatic Ductal Adenocarcinoma, and Colorectal Cancer.
Mcgill University
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
Polaris Pharmaceuticals
Discovery of Novel Oxazepine Derivatives as Akt/ROCK Inhibitors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment.
Zhejiang University
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.
University of Michigan
A close look into the biological and synthetic aspects of fused pyrazole derivatives.
Chengdu University of Traditional Chinese Medicine
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Yantai University
Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
University of Michigan
An ATG4B inhibitor blocks autophagy and sensitizes Sorafenib inhibition activities in HCC tumor cells.
Yantai University
Recent advances in chemistry and bioactivity of marine cyanobacteria Moorea species.
Ningbo University
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
The Johns Hopkins University School of Medicine
Application of the Goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4-tetrahydroisoquinoline inhibitors by beta-fluorination.
University of Kansas
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).
Wuxi Apptec
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.
University of Kansas
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.
University of Alberta Edmonton
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Merck
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
Second Military Medical University
Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain.
Moffitt Cancer Center
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.
Chinese Academy of Sciences
Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives as potential SSRIs.
Sunshine Lake Pharma
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Merck
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
University of Tennessee Health Science Center
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters.
Jagiellonian University Medical College
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine
University of Kansas
Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions.
University of South Florida
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).
Luoxin Pharmaceutical (Shanghai) Co.
Discovery of a novel 53BP1 inhibitor through AlphaScreen-based high-throughput screening.
Yantai University
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.
Hangzhou Xixi Hospital
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein.
TBA
EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.
University of Michigan
High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity.
Jiangsu Normal University
Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
Universities of Shandong
α-Helix-Mimicking Sulfono-γ-AApeptide Inhibitors for p53-MDM2/MDMX Protein-Protein Interactions.
University of South Florida
Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.
National Human Genome Research Institute
Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor.
Merck
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Merck
Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia.
University of South Australia
High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein-Protein Interaction.
Zhejiang University
Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design.
Second Military Medical University
Structural Biology-Inspired Discovery of Novel KRAS-PDEδ Inhibitors.
Second Military Medical University
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Pfizer
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Pfizer
FUSED BICYCLIC SUBSTITUTED N-(1H-INDOL-7-YL)BENZENESULFONAMIDES AND USES THEREOF
Triana Biomedicines
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN
Poseidon Innovation 1
PYRIMIDINE CARBOXAMIDE COMPOUND AND USE THEREOF
Shanghai Meiyue Biotech Development Co.
SERIES OF PIPERIDINE-SUBSTITUTED BENZOIC ACID COMPOUNDS, AND USE THEREOF
Medshine Discovery
Substituted pyrrolo[2,3-d]pyrimidines and pyrazolo[3,4-d]pyrimidines as inhibitors for multi-resistant cancers
Ferris State University
SALT OF DIHYDROPYRIDO[2,3-D]PYRIMIDINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Nanjing Chia Tai Tianqing Pharmaceutical
Broad-spectrum non-covalent coronavirus protease inhibitors
Purdue Research Foundation
Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
Enanta Pharmaceuticals
4-heteroaryl substituted benzoic acid compounds as RORgammaT inhibitors and uses thereof
Merck Sharp & Dohme
Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Vitae Pharmaceuticals
Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
Incyte
Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template.
Ariad Pharmaceuticals
Pharmacological profiles for rat cortical M1 and M2 muscarinic receptors using selective antagonists: comparison with N1E-115 muscarinic receptors.
Mayo Clinic