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Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development

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MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models

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Structure-Based Design of Novel Inhibitors of the MDM2–p53 Interaction

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The MDM2 inhibitor AMG 232 demonstrates robust antitumor efficacy and potentiates the activity of p53-inducing cytotoxic agents

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A phase I study of SAR405838, a novel human double minute 2 (HDM2) antagonist, in patients with solid tumours

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Discovery of a Small Molecule MDM2 Inhibitor (AMG 232) for Treating Cancer

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Phase I Trial of the Human Double Minute 2 Inhibitor MK-8242 in Patients With Advanced Solid Tumors

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SAR405838: A Novel and Potent Inhibitor of the MDM2:p53 Axis for the Treatment of Dedifferentiated Liposarcoma

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TP53 mutations emerge with HDM2 inhibitor SAR405838 treatment in de-differentiated liposarcoma

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Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction

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Rational Design and Binding Mode Duality of MDM2–p53 Inhibitors

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Phase I trial of a novel stapled peptide ALRN-6924 disrupting MDMX- and MDM2-mediated inhibition of WT p53 in patients with solid tumors and lymphomas.

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The p53-MDM2/MDMX axis – A chemotype perspective

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2-Piperidone Type of Chiral Building Block for 3-Piperidinol Alkaloid Synthesis

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Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53–MDM2 interaction with a distinct binding mode

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Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres

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A phase I trial of the human double minute 2 inhibitor (MK-8242) in patients with refractory/recurrent acute myelogenous leukemia (AML)

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<i>MDM2</i> Gene Amplification Is Correlated to Tumor Progression but not to the Presence of SNP309 or <i>TP53</i> Mutational Status in Primary Colorectal Cancers

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Discovery of AM-7209, a Potent and Selective 4-Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction

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Initial Testing (Stage 1) of MK‐8242—A Novel MDM2 Inhibitor—by the Pediatric Preclinical Testing Program

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Phase 1 Dose Escalation Study of MDM2 Inhibitor DS-3032b in Patients with Hematological Malignancies - Preliminary Results

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Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties

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Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2–p53 Interaction

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A phase 1 study of the MDM2 inhibitor DS-3032b in patients (pts) with advanced solid tumors and lymphomas.

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Optimization beyond AMG 232: Discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein–protein interaction

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Pharmacokinetics and metabolism of AMG 232, a novel orally bioavailable inhibitor of the MDM2–p53 interaction, in rats, dogs and monkeys:in vitro–in vivocorrelation

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Targeting Protein-Protein Interactions by Small Molecules

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The Development of New Spirooxindoles Targeting the p53–MDM2 Protein-Protein Interactions for Cancer Therapy

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Abstract B27: A phase I dose escalation study of the MDM2 inhibitor DS-3032b in patients with advanced solid tumors and lymphomas

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Targeting apoptosis in cancer therapy

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Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

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Photoenzymatic enantioselective intermolecular radical hydroalkylation

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Anti-cancer effects of polyphenols via targeting p53 signaling pathway: updates and future directions

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Targeting apoptotic pathways for cancer therapy

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Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives

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Small-molecule MDM2 inhibitors in clinical trials for cancer therapy

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Synthesis of new thiazolo-pyrrolidine–(spirooxindole) tethered to 3-acylindole as anticancer agents

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Design and synthesis of new substituted spirooxindoles as potential inhibitors of the MDM2–p53 interaction

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Development of selective small molecule MDM2 degraders based on nutlin

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Safety and pharmacokinetics of milademetan, a MDM2 inhibitor, in Japanese patients with solid tumors: A phase I study

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Ubiquitin–proteasome system as a target for anticancer treatment—an update

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Network Pharmacology and Bioinformatics Approach Reveals the Therapeutic Mechanism of Action of Baicalein in Hepatocellular Carcinoma

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Recent Progress and Clinical Development of Inhibitors that Block MDM4/p53 Protein–Protein Interactions

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A balancing act: using small molecules for therapeutic intervention of the p53 pathway in cancer

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MDM2/X inhibitors as radiosensitizers for glioblastoma targeted therapy

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p53 regulated senescence mechanism and role of its modulators in age-related disorders

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Stereocontrolled [3+2] Cycloaddition of Donor–Acceptor Cyclopropanes to Iminooxindoles: Access to Spiro[oxindole-3,2′-pyrrolidines]

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Deregulated transcription factors and poor clinical outcomes in cancer patients

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Recent Synthetic Approaches towards Small Molecule Reactivators of p53

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Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators

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Discovery of NewS‐Glycosides andN‐Glycosides of Pyridine‐biphenyl System with Antiviral Activity and Induction of Apoptosis in MCF 7 Cells

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Proteomics for cancer drug design

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Ubiquitin, SUMO, and Nedd8 as Therapeutic Targets in Cancer

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Roles of DANCR/microRNA-518a-3p/MDMA ceRNA network in the growth and malignant behaviors of colon cancer cells

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N‐Alkoxyacrylamides in Domino Reactions: Catalytic and Stereoselective Access to δ‐Lactams

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The expression of MDM2, MDM4, p53 and p21 in myeloid neoplasms and the effect of MDM2/MDM4 dual inhibitor

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Tumor suppressing role of serum-derived exosomal microRNA-15a in osteosarcoma cells through the GATA binding protein 2/murine double minute 2 axis and the p53 signaling pathway

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Direct Lactamization of β‐Arylated δ‐Aminopentanoic Acid Carboxamides: En Route to 4‐aryl‐2‐Piperidones, Piperidines, Antituberculosis Molecule Q203 (Telacebec) and its Analogues

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BindingDB Entry 50021182: Synthesis and biological evaluation of 4-imidazolidinone-containing compounds as potent inhibitors of the MDM2/p53 interaction.

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BindingDB Entry 50018627: Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators.

BindingDB (2024) · UC San Diego · doi:10.7270/q2kp86dp

BindingDB Entry 50018099: Recent Progress and Clinical Development of Inhibitors that Block MDM4/p53 Protein-Protein Interactions.

BindingDB (2024) · UC San Diego · doi:10.7270/q2dv1q2x

BindingDB Entry 50007847: Development of selective small molecule MDM2 degraders based on nutlin.

BindingDB (2021) · UC San Diego · doi:10.7270/q22j6g6h

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