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References from Development of BODIPY FL VH032 as a High-Affinity and Selective von Hippel–Lindau E3 Ligase Fluorescent Probe and Its Application in a Time-Resolved Fluorescence Resonance Energy-Transfer Assay. Local targets link to admitted publications; unresolved targets remain external evidence.
Binding of the von Hippel-Lindau tumor suppressor protein to Elongin B and C
10.1126/science.7660130 · 1995 · External reference
Structure of the VHL-ElonginC-ElonginB complex: implications for VHL tumor suppressor function
10.1126/science.284.5413.455 · 1999 · External reference
The tumour suppressor protein VHL targets hypoxia-inducible factors for oxygen-dependent proteolysis
10.1038/20459 · 1999 · External reference
Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction
10.1021/ja209924v · 2012 · External reference
Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α
10.1002/anie.201206231 · 2012 · External reference
Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface
10.1016/j.chembiol.2012.08.015 · 2012 · External reference
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
10.1021/jm5011258 · 2014 · External reference
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
10.1038/ncomms13312 · 2016 · External reference
Structure of an HIF-1alpha -pVHL complex: hydroxyproline recognition in signaling
10.1126/science.1073440 · 2002 · External reference
Structural basis for the recognition of hydroxyproline in HIF-1 alpha by pVHL
10.1038/nature00767 · 2002 · External reference
Degradation of proteins by PROTACs and other strategies
10.1016/j.apsb.2019.08.001 · 2020 · External reference
Structural basis of PROTAC cooperative recognition for selective protein degradation
10.1038/nchembio.2329 · 2017 · External reference
Selective inhibition of BET bromodomains
10.1038/nature09504 · 2010 · External reference
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)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)
10.1021/acs.jmedchem.7b00675 · 2018 · External reference
3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation
10.1021/jacs.8b05807 · 2018 · External reference
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
10.1021/acs.jmedchem.7b00635 · 2018 · External reference
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
10.1021/acs.jmedchem.8b01413 · 2019 · External reference
Fluorescence polarization assays in small molecule screening
10.1517/17460441.2011.537322 · 2011 · External reference
Development of high throughput screening assays using fluorescence polarization: nuclear receptor-ligand-binding and kinase/phosphatase assays
10.1177/108705710000500204 · 2000 · External reference
A Dual-Readout F2Assay That Combines Fluorescence Resonance Energy Transfer and Fluorescence Polarization for Monitoring Bimolecular Interactions
10.1089/adt.2010.0292 · 2011 · External reference
Fluorescence Polarization (FP) Assays for Monitoring Peptide-Protein or Nucleic Acid-Protein Binding
10.1002/9780470559277.ch090102 · 2009 · External reference
Using TR-FRET to Investigate Protein-Protein Interactions: A Case Study of PXR-Coregulator Interaction
10.1016/bs.apcsb.2017.06.001 · 2018 · External reference
Development of BODIPY FL vindoline as a novel and high-affinity pregnane X receptor fluorescent probe
10.1021/bc5002856 · 2014 · External reference
A vinblastine fluorescent probe for pregnane X receptor in a time-resolved fluorescence resonance energy transfer assay
10.1016/j.ab.2013.09.009 · 2013 · External reference
Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay
10.1021/acs.bioconjchem.0c00507 · 2020 · External reference
Apparent activity in high-throughput screening: origins of compound-dependent assay interference
10.1016/j.cbpa.2010.03.020 · 2010 · External reference
A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors
10.1177/108705710200700102 · 2002 · External reference
Facile Conversion of FP to TR-FRET Assays using Terbium Chelates:Nuclear Receptor Competitive Binding Assays as Examples
10.2174/157018008785777261 · 2008 · External reference
Green/red dual fluorescence detection of total protein and alkaline phosphate-conjugated probes on blotting membranes
10.1002/1522-2683()22:5<896::aid-elps896>3.0.co;2-e · 2001 · External reference
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
10.1002/anie.201507634 · 2016 · External reference
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
10.1073/pnas.1521738113 · 2016 · External reference
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
10.1038/s41467-017-00954-1 · 2017 · External reference
Phthalimide conjugation as a strategy for in vivo target protein degradation
10.1126/science.aab1433 · 2015 · External reference
Kinetics of Amide Formation through Carbodiimide/N-Hydroxybenzotriazole (HOBt) Couplings
10.1021/jo701558y · 2007 · External reference
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
10.1016/0006-2952(73)90196-2 · 1973 · External reference
Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization
10.1016/j.ab.2004.05.055 · 2004 · External reference
Utilization of fluorescence polarization and time resolved fluorescence resonance energy transfer assay formats for SAR studies: Src kinase as a model system
10.1177/1087057104264597 · 2004 · External reference
Inhibition of Bfl-1 with N-aryl maleimides
10.1016/j.bmcl.2010.09.046 · 2010 · External reference
Evaluating PI3 kinase isoforms using Transcreener ADP assays
10.1177/1087057108319864 · 2008 · External reference
Current in vitro high throughput screening approaches to assess nuclear receptor activation
10.2174/138920010794328896 · 2010 · External reference
Early evaluation of compound QT prolongation effects: a predictive 384-well fluorescence polarization binding assay for measuring hERG blockade
10.1016/j.vascn.2006.09.003 · 2007 · External reference
A fluorescence polarization assay for identifying ligands that bind to vascular endothelial growth factor
10.1016/j.ab.2008.03.043 · 2008 · External reference
A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays
10.1177/108705719900400206 · 1999 · External reference
Fluorescence polarization competition assay: the range of resolvable inhibitor potency is limited by the affinity of the fluorescent ligand
10.1177/1087057102239666 · 2003 · External reference
