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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

Alexander Wolf: Molecular Toxicology and PharmacologyGermanyalexander.wolf@helmholtz-muenchen.deAlexander Wolf
Alian Lab. Molecular and Structural VirologyIsraelalian@tx.technion.ac.ilAlian Akram
Angel de Lera group: Chemistry of Retinoids and Epigenetic ModulatorsSpainqolera@uvigo.esAngel R. de Lera
Arndt Group. Organic synthesis.Germanych.enzensperger@gmail.comChristoph Enzensperger
BIOHET. Biologically relevant heterocycles.Spainjosecm@farm.ucm.esJose Carlos Menendez
Bioinformatics and Genetics. Yelekci group.Turkeyyelekci@khas.edu.trKemal YELEKÇİ
Bolognesi's group. Pharmaceutical ChemistryItalymarialaura.bolognesi@unibo.itMaria Laura Bolognesi
Bonger Lab: Biomolecular chemistryNetherlandsk.bonger@science.ru.nlKimberly Bonger
Campiani Group, NatSynDrugs. Drug Discovery and Development Italycampiani@unisi.itGiuseppe Campiani
Campiani Group. Hsp90, HDAC6 and neurodegenerationItalymargherita.brindisi@unisi.itMargherita Brindisi
Cancer Epigenetics SocietyAustriaibennani@b2sg.orgIdriss M. Bennani-Baiti
Christian A. Olsen Group. HDAC inhibitorsDenmarkcao@sund.ku.dkChristian A. Olsen
Conway Group. Chemical and Photochemical Biology, and Synthesis.United Kingdomstuart.conway@chem.ox.ac.ukStuart Conway
DNA Chemical Biology. Clara Brieke group, Dep. Biomolecular MechanismsGermanyClara.Brieke@mpimf-heidelberg.mpg.deClara Brieke
Dekker Group. Medicinal Chemistry.Netherlandsf.j.dekker@rug.nlFrank Dekker
ETAC (Epigenetic Targeting Of Cancer) at MFO (Maison Française d'Oxford)Franceludovic.halby@cnrs.frLudovic Halby
Edelris. Medicinal chemistry companyFranceDidier.roche@edelris.comDidier Roche
EpiDiscoverY. Drug Design and Pharmacology.Denmarkbril@sund.ku.dkBrian Lohse
Epigenetic Med Chem LabItalygsbardella@unisa.itGianluca Sbardella
Filippakopoulos Lab. Protein Science and Structural BiologyUnited Kingdompanagis.filippakopoulos@sgc.ox.ac.ukPanagis Filippakopoulos
Fuchter group. Chemical Synthesis United Kingdomm.fuchter@imperial.ac.ukMatthew Fuchter
Ganesan. Organic Synthesis.United Kingdoma.ganesan@uea.ac.ukArasu Ganesan
Hansen lab (Pharm. and Med. Chemistry)Germanyfinn.hansen@uni-leipzig.deFinn Kristian Hansen
John Gurdon Group. Cell ReprogrammingUnited KingdomMagdalenaKoziol@hotmail.comMagdalena Koziol
Jun. Prof. Olalla Vázquez. Chemical BiologyGermanyvazquezv@staff.uni-marburg.deOlalla Vázquez
Jung group, Chemical epigeneticsGermanymanfred.jung@pharmazie.uni-freiburg.deManfred Jung
Kancera AB Project DirectorSwedenjohan.schultz@kancera.comJohan Schultz
Katarina Nikolic Group. Pharmaceutical Chemistry.Serbiaknikolic@pharmacy.bg.ac.rsKatarina Nikolić
KawamuraUnited Kingdomakane.kawamura@chem.ox.ac.ukakane kawamura
Kolblab Lab. Docking, Chemoinformatics, Molecular dynamicsGermanypeter.kolb@uni-marburg.dePeter Kolb
Kurz group.Germanythomas.kurz@hhu.deThomas Kurz
Magnusdottir Laboratory. Transcriptional Control of Cell StatesIcelanderna@hi.isErna Magnúsdóttir
Mai's GroupItalydante.rotili@uniroma1.itDante Rotili
Maria Duca group - Synthesis and Biomolecular InteractionsFrancemaria.duca@unice.frMaria Duca (WG1)
Martin Group: Medicinal Chemistry & Chemical BiologyNetherlandsn.i.martin@uu.nlNathaniel Martin
Medicinal ChemistrySloveniajanez.ilas@ffa.uni-lj.siIlaš Janez
Medicinal Chemistry groupPortugalfborges@fc.up.ptMaria Fernanda Borges
Mikros group: Biomolecular Spectroscopy & Computational Drug Design GroupGreecemikros@pharm.uoa.grEmmanuel Mikros
Oppermann Group. Epigenetic Mechanisms in Musculoskeletal DiseaseUnited Kingdomudo.oppermann@sgc.ox.ac.ukUdo Oppermann
Organic synthesis and biosensors for epigenetics.Francephilippe.bertrand@univ-poitiers.frPhilippe Bertrand
Paola Arimondo Group: ETAC: PHARMACOCHEMISTRY - CANCER EPIGENETIC REGULATION UNIT Francepaola.arimondo@etac.cnrs.frPaola B. Arimondo
Peter Kele Group. Chemical BiologyHungarykele.peter@ttk.mta.huPéter Kele
Pharmaceutical Chemistry. Sirtuins for Drug Development. Finlandtarja.kokkola@uef.fiTarja Kokkola
Prætorius Group. Modulation of neurotransmission and epigenetic biologyDenmarkrac@sund.ku.dkRasmus Prætorius Clausen
Rome Center for Molecular DesignItalyrino.ragno@uniroma1.itRINO RAGNO
Sippl Lab. Medicinal ChemistryGermanywolfgang.sippl@pharmazie.uni-halle.deWolfgang Sippl
Sirtuin group in Kuopio. Molecular and Protein modelingFinlandMaija.Lahtela-Kakkonen@uef.fiMaija Lahtela-Kakkonen
Structural Bioinformatics & Chemoinformatics.Francepascal.bonnet@univ-orleans.frPascal Bonnet
Viktor Víglaský group. Structure Analysis of BiomacromoleculesSlovakiavviglasky@yahoo.comViktor Víglaský

Cost UE