Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
about
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapyThe structural basis of arrestin-mediated regulation of G-protein-coupled receptorsTargeting MDM2 by the small molecule RITA: towards the development of new multi-target drugs against cancer.Chemical Variations on the p53 Reactivation ThemeFeatures of protein-protein interactions that translate into potent inhibitors: topology, surface area and affinityExpanding the number of 'druggable' targets: non-enzymes and protein-protein interactionsElucidation of Ligand-Dependent Modulation of Disorder-Order Transitions in the Oncoprotein MDM2Crystal Structures of Human MdmX (HdmX) in Complex with p53 Peptide Analogues Reveal Surprising Conformational ChangesStructural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMXUsing a Fragment-Based Approach To Target Protein-Protein InteractionsHalogen-Enriched Fragment Libraries as Leads for Drug Rescue of Mutant p53Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical DevelopmentThe structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutantProtein grafting of p53TAD onto a leucine zipper scaffold generates a potent HDM dual inhibitorThe p53 pathway as a target in cancer therapeutics: obstacles and promiseThe role of p53 in cancer drug resistance and targeted chemotherapyMolecular Mechanisms of p53 Deregulation in Cancer: An Overview in Multiple MyelomaEmerging Non-Canonical Functions and Regulation by p53: p53 and StemnessmRNA Display Selection of an Optimized MDM2-Binding Peptide That Potently Inhibits MDM2-p53 InteractionSimulating molecular mechanisms of the MDM2-mediated regulatory interactions: a conformational selection model of the MDM2 lid dynamicsEnabling large-scale design, synthesis and validation of small molecule protein-protein antagonistsModeling of arylamide helix mimetics in the p53 peptide binding site of hDM2 suggests parallel and anti-parallel conformations are both stable.What can we learn from the evolution of protein-ligand interactions to aid the design of new therapeutics?Probing Difference in Binding Modes of Inhibitors to MDMX by Molecular Dynamics Simulations and Different Free Energy MethodsEnergetic Landscape of MDM2-p53 Interactions by Computational Mutagenesis of the MDM2-p53 InteractionA Strategy for Direct Chemical Activation of the Retinoblastoma ProteinTherapeutic considerations for Mdm2: not just a one trick ponyPatented small molecule inhibitors in the ubiquitin proteasome systemDesign, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions.Targeting p53 for Novel Anticancer Therapy.Privileged diazepine compounds and their emergence as bromodomain inhibitors.Chemical genetics.Pathological unfoldomics of uncontrolled chaos: intrinsically disordered proteins and human diseasesA computational analysis of the binding model of MDM2 with inhibitors.Design and Synthesis of Functionalized Trisaccharides as p53-Peptide Mimics.Chronic inflammation and cancer: potential chemoprevention through nuclear factor kappa B and p53 mutual antagonismReversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteinsIn silico identification of an interferon inhibitor.Application of a sequential multicomponent assembly process/huisgen cycloaddition strategy to the preparation of libraries of 1,2,3-triazole-fused 1,4-benzodiazepines.From laptop to benchtop to bedside: structure-based drug design on protein targets.
P2860
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P2860
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
description
2005 nî lūn-bûn
@nan
2005 թուականի Փետրուարին հրատարակուած գիտական յօդուած
@hyw
2005 թվականի փետրվարին հրատարակված գիտական հոդված
@hy
2005年の論文
@ja
2005年論文
@yue
2005年論文
@zh-hant
2005年論文
@zh-hk
2005年論文
@zh-mo
2005年論文
@zh-tw
2005年论文
@wuu
name
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@ast
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@en
type
label
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@ast
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@en
prefLabel
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@ast
Discovery and cocrystal struct ...... ts that activate p53 in cells.
@en
P2093
P356
P1476
Discovery and cocrystal struct ...... sts that activate p53 in cells
@en
P2093
Anna C Maroney
Bruce E Tomczuk
Bruce L Grasberger
Carl L Manthey
Carol F Franks
Carsten Schubert
Daniel J Parks
Diane Maguire
Eugene C Petrella
Gwendolyn R Bylebyl
P304
P356
10.1021/JM049137G
P407
P577
2005-02-01T00:00:00Z