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
Auvray M., Bolze F., Clavier G., Mahuteau-Betzer F. (2021 Jan 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 : https://doi.org/10.1016/j.dyepig.2020.109083Year of publication 2020
Yu Luo, Anton Granzhan, Daniela Verga, Jean-Louis Mergny (2020 Dec 28)
FRET-MC: A fluorescence melting competition assay for studying G4 structures in vitro.
Biopolymers : Early view : bip23415 : DOI : 10.1002/bip.23415Year of publication 2021
Oksana Reznichenko, Anne Cucchiarini, Valérie Gabelica, Anton Granzhan (2020 Dec 8)
Quadruplex DNA-guided ligand selection from dynamic combinatorial libraries of acylhydrazones
Organic and Biomolecular Chemistry : 19 : 379-386 : DOI : 10.1039/D0OB01908AYear of publication 2020
Lei He, Zhenyu Meng, Qianqian Guo, Xiangyang Wu, Marie-Paule Teulade-Fichou, Edwin Kok Lee Yeow, Fangwei Shao (2020 Nov 28)
Fluorogenic Pt complexes distinguish the quantity and folding behavior of RNA G-quadruplexes between live cancerous and healthy cells.
Chemical communications (Cambridge, England) : 56 : 14459-14462 : DOI : 10.1039/d0cc05622g
Leduc A., Chaouni S., De marzi L., Pouzoulet F., Mégnin-Chanet F., Stephan D., Habrand J.L., Sichel F., Laurent C. (2020 Nov 24)
Biological Effects of Scattered Versus Scanned Proton Beams on Normal Tissues in Total Body Irradiated Mice: Survival, Genotoxicity, Oxidative Stress and Inflammation
Antioxidants : 9 : 1170 : DOI : 10.3390/antiox9121170
Anouchka Gatin, Isabelle Billault, Patricia Duchambon, Guillaume Van der Rest, Cécile Sicard-Roselli (2020 Nov 20)
