137 articles for thisTarget
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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
Rational design and synthesis of 1,5-disubstituted tetrazoles as potent inhibitors of the MDM2-p53 interaction.
Jagiellonian University
Discovery of novel polycyclic spiro-fused carbocyclicoxindole-based anticancer agents.
Sichuan University and Collaborative Innovation Center For Biotherapy
Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas.
University of Pisa
Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.
Merck Research Laboratories
Peptide-based inhibitors of protein-protein interactions.
Wroclaw University of Technology
Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin.
University of East Anglia
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Novartis Institutes For Biomedical Research
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
University of Michigan Comprehensive Cancer Center and Departments of Internal Medicine
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Amgen
Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor.
Daiichi Sankyo
Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
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
Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
Merck Research Laboratories
Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy.
Second Military Medical University
Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
Chinese Academy of Medical Science and Peking Union Medical College
Hot spot-based design of small-molecule inhibitors for protein-protein interactions.
University of Utah
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.
Novartis Institutes For Biomedical Research
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Amgen
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
Merck Research Laboratories
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Amgen
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.
Roche Pharma Research
5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.
University of Nottingham
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
Roche Research Center
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
University of Michigan
Affinity-based screening of MDM2/MDMX-p53 interaction inhibitors by chemical array: identification of novel peptidic inhibitors.
Kyoto University
Functional consequences of retro-inverso isomerization of a miniature protein inhibitor of the p53-MDM2 interaction.
Southwest University
Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2.
University of Pittsburgh
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Roche Research Center
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
University of Texas At Houston
Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
TBA
Chemical modulators working at pharmacological interface of target proteins.
Korea University College of Pharmacy Sejong-Ro
Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
Daiichi Sankyo
AM-8553: a novel MDM2 inhibitor with a promising outlook for potential clinical development.
University of Michigan Comprehensive Cancer Center
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.
Novartis Institutes For Biomedical Research
Unbiased binding assays for discovering small-molecule probes and drugs.
Broad Institute of Harvard and Mit
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
Yale University
NMR screening for lead compounds using tryptophan-mutated proteins.
Institute For Biochemistry
Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.
University of California San Francisco
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
Newcastle University
Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
State University of New York
Functional profiling of p53-binding sites in Hdm2 and Hdmx using a genetic selection system.
Purdue University
Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.
University of Michigan
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Amgen
Discovery of new pyridoacridine alkaloids from Lissoclinum cf. badium that inhibit the ubiquitin ligase activity of Hdm2 and stabilize p53.
National Cancer Institute-Frederick
Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression.
TBA
2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry.
Xinjiang Technical Institute of Physics and Chemistry
Natural spirocyclic alkaloids and polyphenols as multi target dementia leads.
Rmit University
Recent applications of covalent chemistries in protein-protein interaction inhibitors.
University of Maryland
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.
Second Military Medical University
Recent Progress and Clinical Development of Inhibitors that Block MDM4/p53 Protein-Protein Interactions.
University of Chinese Academy of Sciences
Diversity-oriented synthesis as a tool to expand the chemical space of DNA-encoded libraries.
University of Florence
Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells.
Shanghai Institute of Materia Medica
Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Yancheng Teachers University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
Stapled peptides as scaffolds for developing radiotracers for intracellular targets: Preliminary evaluation of a radioiodinated MDM2-binding stapled peptide in the SJSA-1 osteosarcoma model.
Duke University Medical Center
Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond.
China Pharmaceutical University
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Cyclic Peptide Screening Methods for Preclinical Drug Discovery.
University of Washington
Discovery of MDM2-p53 and MDM4-p53 protein-protein interactions small molecule dual inhibitors.
Universidade De Lisboa
Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries.
University of Wisconsin-Madison
Design, synthesis, and biological evaluation of nitroisoxazole-containing spiro[pyrrolidin-oxindole] derivatives as novel glutathione peroxidase 4/mouse double minute 2 dual inhibitors that inhibit breast adenocarcinoma cell proliferation.
Chengdu University of Traditional Chinese Medicine
Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions.
University of South Florida
hDM2 protein-binding peptides screened from stapled ?-helical peptide phage display libraries with different types of staple linkers.
Tokyo Institute of Technology
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.
St. John'S University
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
University of Naples "Federico Ii
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
Shaanxi University of Science & Technology
Enhancing the Cell Permeability of Stapled Peptides with a Cyclic Cell-Penetrating Peptide.
The Ohio State University
Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
University of Groningen
Development of selective small molecule MDM2 degraders based on nutlin.
University of Wisconsin-Madison
The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.
Sichuan University
?-Helix-Mimicking Sulfono-?-AApeptide Inhibitors for p53-MDM2/MDMX Protein-Protein Interactions.
University of South Florida
Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.
TBA
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like ?-Helical Mimetics.
Dalian University of Technology
2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists.
University of Groningen
Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold.
Daiichi Sankyo
Hexylitaconic acid: a new inhibitor of p53-HDM2 interaction isolated from a marine-derived fungus, Arthrinium sp.
Kanazawa University
The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy.
International Institute For Translational Chinese Medicine
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.
Novartis Institutes For Biomedical Research
Role of p53 circuitry in tumorigenesis: A brief review.
Jss Academy of Higher Education and Research
Unique arginine array improves cytosolic localization of hydrocarbon-stapled peptides.
Yale University
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
East China University of Science and Technology
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
University of Naples Federico II
1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
Jagiellonian University
d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions.
University of Maryland
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
East China University of Science & Technology
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
University of Naples Federico II
Investigation of the inhibitory mechanism of apomorphine against MDM2-p53 interaction.
Kyoto University
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2 Pyridyl]Amino]Pyrazine-2-carbonitrile and therapeutic uses thereof
Cancer Research Technology
Method for controlling hematophagous or sap-feeding arthropods
Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
Thienopyridine carboxamides as ubiquitin-specific protease inhibitors
Valo Early Discovery
Compounds antagonizing A3 adenosine receptor, method for preparing them, and medical-use thereof
Handok
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof
Cancer Research Technology
2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
Lycera
Aromatic heterocyclic compounds and their application in pharmaceuticals
Sunshine Lake Pharma
AMPK-activating heterocyclic compounds and methods for using the same
Rigel Pharmaceuticals
γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
Novassay
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
Wyeth Research
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Schering-Plough Research Institute
Identification and characterization of new inhibitors of fungal homoserine kinase.
Mcmaster University
Cloning and functional expression of cDNAs encoding human and rat pancreatic polypeptide receptors.
Amgen
Synthesis and structure-activity relationship of the isoindolinyl benzisoxazolpiperidines as potent, selective, and orally active human dopamine D4 receptor antagonists.
Aventis Pharmaceuticals
Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity.
Janssen Research Foundation
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.
University of Pittsburgh
Sequential mechanism of assembly of multidrug efflux pump AcrAB-TolC.
University of Oklahoma
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
Nci-Fcrdc
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.
Daiichi Asubio Medical Research Laboratories
Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions.
Universita Degli Studi Di Firenze
Structure-based optimization of novel azepane derivatives as PKB inhibitors.
Roche Diagnostics