
Structural biology of epigenetic targets
Structural biology of epigenetic targets
Chromatin structure is a major barrier to all nuclear processes and its modulation is essential for correct cell growth. There is now clear evidence that defects in chromatin modulation are responsible for a wide range of diseases, including cancer. Epigenetic modifications have a large impact on chromatin structure, acting in synergy with ATP-dependent remodelers, histone variants and histone chaperones to regulate nuclear mechanisms. By combining state-of-the-art biochemical and crystallographic techniques, we aim to understand chromatin remodeling at the molecular level. Three main targets are the current focus of our research: protein arginine methyltransferases (PRMTs), histone chaperones and histone deacetylases (HDACs). Furthermore, we are also developing structurebased rational approaches to characterize small molecule modulators of the biological activities of our targets since they are frequently involved in human diseases. Our team also participates in collaborative research on several related projects which require our specific expertise. Present collaborations concern the structural studies of complexes of cancer-related targets such as the Translationally Controlled Tumor Protein (TCTP) and the mRNA of human histone H4.
Members
Researchers
Engineers
Publications
2022
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach
- Giulia Iannelli
- Ciro Milite
- Nils Marechal
- Vincent Cura
- Luc Bonnefond
- Nathalie Troffer-Charlier
- Alessandra Feoli
- Donatella Rescigno
- Yalong Wang
- Alessandra Cipriano
- Monica Viviano
- Mark Bedford
- Jean Cavarelli
- Sabrina Castellano
- Gianluca Sbardella
Journal of Medicinal Chemistry ; Volume: 65 ; Page: 11574-11606
Insect Cells-Baculovirus System for the Production of Difficult to Express Proteins: From Expression Screening for Soluble Constructs to Protein Quality Control
- Simon Pichard
- Nathalie Troffer-Charlier
- Isabelle Kolb-Cheynel
- Pierre Poussin-Courmontagne
- Wassim Abdulrahman
- Catherine Birck
- Vincent Cura
- A. Poterszman
Insoluble Proteins ; Volume: 2406 ; Page: 281-317
HR-Bac, a toolbox based on homologous recombination for expression, screening and production of multiprotein complexes using the baculovirus expression system
- Olga Kolesnikova
- Amélie Zachayus
- Simon Pichard
- Judit Osz
- Natacha Rochel
- Paola Rossolillo
- Isabelle Kolb-Cheynel
- Nathalie Troffer-Charlier
- Emmanuel Compe
- Olivier Bensaude
- Imre Berger
- Arnaud Poterszman
Scientific Reports ; Volume: 12 ; Page: 2030
2021
Structure, Activity and Function of the PRMT2 Protein Arginine Methyltransferase
- Vincent Cura
- Jean Cavarelli
Life ; Volume: 11 ; Page: 1263
2020
FFAT motif phosphorylation controls formation and lipid transfer function of inter‐organelle contacts
- Thomas Di Mattia
- Arthur Martinet
- Souade Ikhlef
- Alastair G Mcewen
- Yves Nominé
- Corinne Wendling
- Pierre Poussin‐courmontagne
- Laetitia Voilquin
- Pascal Eberling
- Frank Ruffenach
- Jean Cavarelli
- John Slee
- Timothy P Levine
- Guillaume Drin
- Catherine Tomasetto
- Fabien Alpy
EMBO Journal ; Volume: 39
Aminobenzosuberone derivatives as PfA-M1 inhibitors: Molecular recognition and antiplasmodial evaluation
- Emmanuel Salomon
- Marjorie Schmitt
- Elisabeth Mouray
- Alastair G Mcewen
- Lotfi Bounaadja
- Morgan Torchy
- Pierre Poussin-Courmontagne
- Sarah Alavi
- Céline Tarnus
- Jean Cavarelli
- Isabelle Florent
- Sebastien Albrecht
Bioorganic Chemistry ; Volume: 98 ; Page: 103750
2018
Role of the SMN complex and the methylosome in selenoprotein mRNP assembly and translation
- Anne-Sophie Gribling-Burrer
- Hassan Hayek
- Vincent Cura
- Martine Barkats
- Jean Cavarelli
- Séverine Massenet
- Franck Martin
- Gilbert Eriani
- Christine Allmang
Hijacking DNA methyltransferase transition state analogues to produce chemical scaffolds for PRMT inhibitors
- Ludovic Halby
- Nils Marechal
- Dany Pechalrieu
- Vincent Cura
- Don-Marc Franchini
- Céline Faux
- Frédéric Alby
- Nathalie Troffer-Charlier
- Srikanth Kudithipudi
- Albert Jeltsch
- Wahiba Aouadi
- Etienne Decroly
- Jean-Claude Guillemot
- Patrick Page
- Clotilde Ferroud
- Luc Bonnefond
- Dominique Guianvarc'H
- Jean Cavarelli
- Paola Arimondo
Philosophical Transactions of the Royal Society B: Biological Sciences ; Volume: 373 ; Page: 20170072
2017
SECIS-binding protein 2 interacts with the SMN complex and the methylosome for selenoprotein mRNP assembly and translation
- Anne-Sophie Gribling-Burrer
- Michael Leichter
- Laurence Wurth
- Alexandra Huttin
- Florence Schlotter
- Nathalie Troffer-Charlier
- Vincent Cura
- Martine Barkats
- Jean Cavarelli
- Séverine Massenet
- Christine Allmang
Nucleic Acids Research ; Volume: 45 ; Page: 5399-5413
Insight into the remarkable affinity and selectivity of the aminobenzosuberone scaffold for the M1 aminopeptidases family based on structure analysis
- G Peng
- A Mcewen
- V Olieric
- Céline Schmitt
- Sébastien Albrecht
- Jean Cavarelli
- Celine Tarnus
Proteins ; Volume: 85 ; Page: 1413-1421