Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

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Targeting Protein-Protein Interactions in the HIF System Cyclic and Macrocyclic Peptides as Chemical Tools To Recognise Protein Surfaces and Probe Protein-Protein Interactions Surfing the Protein-Protein Interaction Surface Using Docking Methods: Application to the Design of PPI Inhibitors Targeting protein function: the expanding toolkit for conditional disruption Discovery of novel inhibitors disrupting HIF-1α/von Hippel-Lindau interaction through shape-based screening and cascade docking Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation.Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.Induced protein degradation: an emerging drug discovery paradigm.Insights into Cullin-RING E3 ubiquitin ligase recruitment: structure of the VHL-EloBC-Cul2 complex Ligand deconstruction: Why some fragment binding positions are conserved and others are not Serendipitous SAD Solution for DMSO-Soaked SOCS2-ElonginC-ElonginB Crystals Using Covalently Incorporated Dimethylarsenic: Insights into Substrate Receptor Conformational Flexibility in Cullin RING Ligases.Structural basis of PROTAC cooperative recognition for selective protein degradation Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors LDL suppresses angiogenesis through disruption of the HIF pathway via NF-κB inhibition which is reversed by the proteasome inhibitor BSc2118.Focused grid-based resampling for protein docking and mapping.Structure-Guided Design of Peptides as Tools to Probe the Protein-Protein Interaction between Cullin-2 and Elongin BC Substrate Adaptor in Cullin RING E3 Ubiquitin Ligases Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Crystal Structure of the Cul2-Rbx1-EloBC-VHL Ubiquitin Ligase Complex.Chemical Methods to Knock Down the Amyloid Proteins.Drugging the undruggable: targeting challenging E3 ligases for personalized medicine.Targeted Protein Degradation by Small Molecules.Targeted Protein Degradation: from Chemical Biology to Drug Discovery.Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras.Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions.Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders.Pred-binding: large-scale protein-ligand binding affinity prediction.QSAR modeling and in silico design of small-molecule inhibitors targeting the interaction between E3 ligase VHL and HIF-1α.Thioamide substitution to probe the hydroxyproline recognition of VHL ligands.Design, Synthesis, and Characterization of Brequinar Conjugates as Probes to Study DHODH Inhibition.Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets.Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation

P2860

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P2860

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

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2014 nî lūn-bûn

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2014 թուականի Հոկտեմբերին հրատարակուած գիտական յօդուած

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2014 թվականի հոտեմբերին հրատարակված գիտական հոդված

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2014年の論文

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