Development of novel small molecules to target cellular pathways

DOI

Small molecules represent powerful tools to dissect physiological and pathological states of signaling pathways, yet require characterization through X-ray crystallography. This proposal encompasses the investigation of new classes of small molecules that target difficult proteins and non-typical binding sites. This includes the development of supramolecular compounds or cyclic peptides to address “non-druggable" proteins. The main collaborative research fields are tackling Ras protein signaling with structure-guided ligand design, developing inhibitors of the Ras-binding protein PDEd, screening of a novel sp3-enriched fragment library or targeting genetic regulators. Cellular signaling will also be addressed through the structural analysis of deubiquitinating enzymes or regulators of the kinetochore. Finally, we plan to crystallize membrane proteins including GPCRs in order to understand their biological function, characterize their ligand specificity and develop novel regulators.

Identifier
DOI https://doi.org/10.15151/ESRF-ES-2025026699
Metadata Access https://icatplus.esrf.fr/oaipmh/request?verb=GetRecord&metadataPrefix=oai_datacite&identifier=oai:icatplus.esrf.fr:inv/2025026699
Provenance
Creator Dihia MOUSSAOUI ORCID logo; Matthias MÜLLER ORCID logo; Andrea SCRIMA (ORCID: 0000-0003-2760-611X); Danilo DANGELO ORCID logo; Janina NIGGENABER (ORCID: 0000-0003-2942-263X); Raphael GASPER-SCHOENENBRUECHER ORCID logo
Publisher ESRF (European Synchrotron Radiation Facility)
Publication Year 2028
Rights CC-BY-4.0; https://creativecommons.org/licenses/by/4.0
OpenAccess true
Representation
Resource Type Data from large facility measurement; Collection
Discipline Particles, Nuclei and Fields