153 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.
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
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 JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
Shanghai Institute of Materia Medica
Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer.
Nanjing University of Chinese Medicine
Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development.
Aileron Therapeutics
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2-p53 Inhibitor.
Unnatural Products
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 α-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
α-Helix-Mimicking Sulfono-γ-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 α-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
NEW SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS
Boehringer Ingelheim International
Substituted pyrrolo[3,4-d]imidazoles as MDM2-p53 inhibitors
Luoxin Pharmaceutical (Shanghai)
CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
Amgen
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors
Boehringer Ingelheim International
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
Boehringer Ingelheim International
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
Boehringer Ingelheim International
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
Boehringer Ingelheim International
Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity
Astex Therapeutics
Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
Amgen
A Unique Mdm2-Binding Mode of the 3-Pyrrolin-2-one- and 2-Furanone-Based Antagonists of the p53-Mdm2 Interaction.
Jagiellonian University
Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
Novartis
A facile one-pot synthesis of 2-arylamino-5-aryloxylalkyl-1,3,4-oxadiazoles and their urease inhibition studies.
Mirpur University of Science and Technology (Must)
Inhibition of arginine aminopeptidase by bestatin and arphamenine analogues. Evidence for a new mode of binding to aminopeptidases.
University of Wisconsin
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.
Johnson & Johnson Pharmaceutical
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Johnson & Johnson Pharmaceutical
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity.
Johnson & Johnson Pharmaceutical
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
Johnson & Johnson Pharmaceutical
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.
Virginia Commonwealth University
Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53.
Max Planck Institute
Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
H. Lee Moffitt Cancer Center
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.
University of Newcastle Upon Tyne
Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction.
Schering-Plough Research Institute
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
University of Michigan