Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development - Wikidata - awgldk - TriplyDB

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

http://www.wikidata.org/entity/Q27684199

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Chemical Variations on the p53 Reactivation Theme Modulation of Protein-Protein Interactions for the Development of Novel Therapeutics Deconstruction of a Nutlin: Dissecting the Binding Determinants of a Potent Protein–Protein Interaction Inhibitor Significant Differences in the Development of Acquired Resistance to the MDM2 Inhibitor SAR405838 between In Vitro and In Vivo Drug Treatment Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2-p53 and MDMX-p53 protein-protein interactions†Electronic supplementary information (ESI) available: Experimental details for compound synthesis, analytical data for all compounds and in 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 Organocatalytic, diastereo- and enantioselective synthesis of nonsymmetric cis-stilbene diamines: a platform for the preparation of single-enantiomer cis-imidazolines for protein-protein inhibition.Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction.Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions.Induced protein degradation: an emerging drug discovery paradigm.Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach.Selective and potent proteomimetic inhibitors of intracellular protein-protein interactions Small-molecule MDM2-p53 inhibitors: recent advances.Alternative modulation of protein-protein interactions by small molecules Targeting protein-protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?State-of-the-art strategies for targeting protein-protein interactions by small-molecule inhibitors.Derivatives of Procaspase-Activating Compound 1 (PAC-1) and their Anticancer Activities.How To Design a Successful p53-MDM2/X Interaction Inhibitor: A Thorough Overview Based on Crystal Structures.Inhibition of the p53/hDM2 protein-protein interaction by cyclometallated iridium(III) compounds.Redox effects and cytotoxic profiles of MJ25 and auranofin towards malignant melanoma cells.The MDM2 small-molecule inhibitor RG7388 leads to potent tumor inhibition in p53 wild-type neuroblastoma Results of the Phase I Trial of RG7112, a Small-Molecule MDM2 Antagonist in Leukemia.Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas Targeting ubiquitination for cancer therapies.Preparation of (-)-Nutlin-3 using enantioselective organocatalysis at decagram scale.Oncogenic protein interfaces: small molecules, big challenges.Resistance acquisition to MDM2 inhibitors.Pharmacological reactivation of p53 as a strategy to treat cancer.The clinical and therapeutic uses of MDM2 and PSMA and their potential interaction in aggressive cancers.Targeting the MDM2-p53 Protein-Protein Interaction for New Cancer Therapy: Progress and Challenges.Reactivation of p53 via MDM2 inhibition.Medicinal Chemistry Strategies to Disrupt the p53-MDM2/MDMX Interaction.Pharmacological activation of wild-type p53 in the therapy of leukemia.Reviving the guardian of the genome: Small molecule activators of p53.Structure- and ligand-based virtual screening identifies new scaffolds for inhibitors of the oncoprotein MDM2.The use of ion mobility mass spectrometry to probe modulation of the structure of p53 and of MDM2 by small molecule inhibitors Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.Combination treatment with rucaparib (Rubraca) and MDM2 inhibitors, Nutlin-3 and RG7388, has synergistic and dose reduction potential in ovarian cancer.

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

http://www.wikidata.org/entity/Q27684199

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2013 nî lūn-bûn

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2013 թուականի Մայիսին հրատարակուած գիտական յօդուած

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2013 թվականի մայիսին հրատարակված գիտական հոդված

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2013年の論文

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年学术文章

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2013年學術文章

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name

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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type

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

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Allen Lovey

http://www.w3.org/2001/XMLSchema#string

Binh Vu

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Bradford Graves

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Christian Tovar

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Chunlin Zhao

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Giacomo Pizzolato

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Jin-Jun Liu

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Kathryn Packman

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Kelli Glenn

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Lyubomir Vassilev

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P2860

Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain

In vivo activation of the p53 pathway by small-molecule antagonists of MDM2

Structure-based design of novel inhibitors of the MDM2-p53 interaction

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

Regulation of p53 stability by Mdm2

p53, the cellular gatekeeper for growth and division

Surfing the p53 network

Functions of the MDM2 oncoprotein

The mdm-2 oncogene product forms a complex with the p53 protein and inhibits p53-mediated transactivation

The p53 pathway: positive and negative feedback loops

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10.1021/ML4000657

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Aagianik kimischri

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4027145

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