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New publication of COSM group : “New Triazacycloalkane Derivatives as Cytotoxic Agents for CLL Treatment: From Proof of Concept to the Targeting Biomolecule”

Axia Marlin, Fiona Le Pape, Jocelyn Le Goff, Nadège Hamon, Thibault Troadec, Raphaël Tripier, Christian Berthou, and Véronique Patinec

DOI: 10.1021/acs.bioconjchem.2c00227

The no3py ligand and its bifunctional analogue no3pyCOOK were synthesized to investigate their action toward zinc(II) depletion related to the apoptosis phenomenon in chronic lymphocytic leukemia (CLL) cells. no3py was used as the “free” ligand, while its “graftable” derivative was conjugated on a newly synthesized bifunctional sialoglycan, 6′-SL-NH2, selected to specifically bind CD22 biomarker expressed on the B-CLL cell surface. Biological in vitro studies of no3py and 6′-SL-no3py consisting of real-time detection of cell health (cytotoxicity and proliferation) and caspases 3/7 activation (crucial enzymes whose activation triggers cell death signaling pathways) have been investigated.