UMR9187 / U1196 – Chemistry and Modelling for the Biology of Cancer (CMBC)

The central activity of the CMBC unit is to develop small molecules to probe and control the biological activities of key targets involved in cancer. These are non B-nucleic acid structures (G-quadruplexes, Abasic sites, …) and proteins (TAM kinases, non B-nucleic acid structures interacting proteins, …).

The drug and probe discovery activity is sustained by molecular modelling approaches and imaging. The CMBC unit is hosting the Institut Curie–CNRS proprietary library comprised of over 9000 chemical compounds.

The main research themes of the unit include:

  • Design and synthesis of G-quadruplex targeting agents for probing, imaging and mapping
  • Design, synthesis and studies of novel small-molecule ligands and probes able to recognize unusual DNA and RNA structures
  • Screening approaches and rational design for the synthesis of kinase inhibitors
  • Identificaction of radiosensitizing molecules for the treatment of cancers and determination of their molecular mechanisms of action

The main methodological approaches are :

  • Chemical biology
  • Medicinal chemistry (Hit to lead optimization)
  • Biophysics and Biochemistry of nucleic acids
  • Molecular dynamics and virtual screening
  • Cellular biology & radiosensitization

Key publications

Year of publication 2021

Anouchka Gatin, Isabelle Billault, Patricia Duchambon, Guillaume Van der Rest, Cécile Sicard-Roselli (2022 Jan 3)

Oxidative radicals (HO or N3) induce several di-tyrosine bridge isomers at the protein scale.

Free radical biology & medicine : 162 : 461-470 : DOI : 10.1016/j.freeradbiomed.2020.10.324
Abegão L.M., Santos F.A., Piguel S., Rodrigues J.J., Mendonça C.R., De Boni L. (2021 Apr 15)

The ability of 2,5-disubstituted oxazole dyes derivatives to generate two-photon upconversion photoluminescence and its brightness evaluation

Journal of Photochemistry and Photobiology A: Chemistry : 411 : 113214 : DOI : 10.1016/j.jphotochem.2021.113214
Elisa Le Boiteux, Franck Court, Pierre-Olivier Guichet, Catherine Vaurs-Barrière, Isabelle Vaillant, Emmanuel Chautard, Pierre Verrelle, Bruno M Costa, Lucie Karayan-Tapon, Anne Fogli, Philippe Arnaud (2021 Mar 15)

Widespread overexpression from the four DNA hypermethylated HOX clusters in aggressive (IDHwt) glioma is associated with H3K27me3 depletion and alternative promoter usage.

Molecular oncology : Accepted article : DOI : 10.1002/1878-0261.12944
Alexandre Leduc, Samia Chaouni, Frédéric Pouzoulet, Ludovic De Marzi, Frédérique Megnin-Chanet, Erwan Corre, Dinu Stefan, Jean-Louis Habrand, François Sichel, Carine Laurent (2021 Mar 13)

Differential normal skin transcriptomic response in total body irradiated mice exposed to scattered versus scanned proton beams.

Scientific reports : 11 : 5876 : DOI : 10.1038/s41598-021-85394-0
Auvray M., Bolze F., Clavier G., Mahuteau-Betzer F. (2021 Mar 1)

Silafluorene as a promising core for cell-permeant, highly bright and two-photon excitable fluorescent probes for live-cell imaging

Dyes and Pigments : 187 : 109083 : DOI : 10.1016/j.dyepig.2020.109083
Thomas Barbot, Veronica Beswick, Cédric Montigny, Éric Quiniou, Nadège Jamin and Liliane Mouawad (2021 Feb 4)

Deciphering the mechanism of inhibition of SERCA1a by sarcolipin using molecular simulations

Frontiers in Molecular Biosciences : 7 : 606254 : DOI : 10.3389/fmolb.2020.606254