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WG1 Epigenetic Chemical Probes

Focus

Organic synthesis for chemical biology and medicinal chemistry applications:

  • Synthesis of compound libraries targeting specific epigenetic enzymes or protein-protein interaction domains.
  • Lead optimization of initial hits to the point where they can be used as selective chemical probes or developed further as candidates for preclinical drug discovery.
  • New methods that target chromatin in a loci-specific manner to up or downregulate specific genes.

Workplan

  1. Synthesis of DNA methyltransferase inhibitors with novel scaffolds that are not nucleoside-based.
  2. Synthesis of isoform-selective HDAC inhibitors.
  3. Synthesis of small molecule HAT inhibitors.
  4. Synthesis of KMT inhibitors that are selective for specific family members.
  5. Synthesis of KDM1 inhibitors, both reversible and irreversible, with selectivity over MAO.
  6. Synthesis of Jumonji KDM inhibitors with subtype selectivity.
  7. Synthesis of PRMT inhibitors.
  8. Synthesis of selective bromodomain ligands.
  9. Small molecule ligands for Tudor and PHD domains.
  10. Small molecule modulators of miRNA expression.

Coordinator

  • Dr. Paola B. ARIMONDO
  • USR 3388 Epigenetic Targeting of Cancer -ETaC- CNRS-Pierre Fabre CRDPF
  • 3 avenue Hubert Curien - 31 035 TOULOUSE CEDEX 01 - Francez
  • Mail. paola.arimondo@etac.cnrs.fr

Working Groups Members


Cost UE