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)

Search results

• Finished

  Molecular and Cellular Biology PhD Programme (4 Year PhD)

  Owen-Hughes, T. (Investigator)

  2/09/13 → 1/09/17

  Project: Research

  • Von Hippel-Lindau 100%
  • Procollagen-Proline Dioxygenase 66%
  • Hypoxia-Inducible Factors 66%
  • Protein Catabolism 55%
  • VH298 45%

• DrugE3CRL's: Probing Druggability of Multisubunit Complexes: E3 Cullin RING Ligases (ERC Starting Grant)

  Ciulli, A. (Investigator)

  COMMISSION OF THE EUROPEAN COMMUNITIES

  1/05/13 → 30/04/18

  Project: Research

  • Protein Catabolism 100%
  • Proteolysis Targeting chimera (PROTAC) 96%
  • Ubiquitin-Conjugating Enzyme 83%
  • Ligase 67%
  • Von Hippel-Lindau 60%

• Dissecting and Exploiting Molecular Recognition at Protein-Protein Interfaces (David Phillips Fellowship)

  Ciulli, A. (Investigator)

  Biotechnology and Biological Sciences Research Council

  8/04/13 → 7/07/15

  Project: Research

  • Chemical Probes 100%
  • Small Molecule 95%
  • Ubiquitin-Conjugating Enzyme 93%
  • Bromodomain 83%
  • Small Molecules 53%

• Design of Orthogonal Molecular Probes Targeting Engineered Von-Hippel Lindau (VHL) E3 Ubiquitin Ligase for the Control of Intercellular Protein Levels

  Ciulli, A. (Investigator)

  COMMISSION OF THE EUROPEAN COMMUNITIES

  8/04/13 → 7/04/15

  Project: Research

  • Hypoxia-Inducible Factors 100%
  • Von Hippel-Lindau 94%
  • Hypoxia Inducible Factor 68%
  • Small Molecule 67%
  • E3 Ubiquitin Ligase 63%

• Strategic Award: Wellcome Trust Technology Platform

  Blow, J. (Investigator), Lamond, A. (Investigator) & Owen-Hughes, T. (Investigator)

  1/01/13 → 30/09/18

  Project: Research

  • Proteomics 100%
  • Ubiquitin 96%
  • Proteome 70%
  • Messenger RNA 59%
  • Chromatin 59%

• A Translational Engine for Biomedical Discoveries (Strategic Grant)

  Fairlamb, A. (Investigator) & Gilbert, I. (Investigator)

  1/01/13 → 30/09/15

  Project: Research

  • Proteolysis Targeting chimera (PROTAC) 100%
  • Protein Catabolism 87%
  • Visceral Leishmaniasis 73%
  • Trypanosoma Brucei 67%
  • Ubiquitin-Conjugating Enzyme 64%

• Mechanisms of Inflammation and Hypoxia-Induced Responses Mediated by HIF and NF-KB in Cancer (Senior Research Fellowship)

  Lamond, A. (Investigator) & Rocha, S. (Investigator)

  1/08/11 → 1/08/17

  Project: Research

  • Von Hippel-Lindau 100%
  • Procollagen-Proline Dioxygenase 66%
  • Hypoxia-Inducible Factors 66%
  • Protein Catabolism 55%
  • Hypoxia Response 53%