Cover Feature: Improving Affinity while Reducing Kidney Uptake of CXCR4-Targeting Radioligands Derived from the Endogenous Antagonist EPI-X4 (ChemMedChem 6/2025)
Dr. Raghuvir H. Gaonkar, Dr. Thibaud Bailly, Dr. Jacopo Millul, Dr. Rosalba Mansi, Dr. Mirja Harms, Prof. Dr. Jan Münch, Prof. Dr. Melpomeni Fani
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Abstract
This cover art highlights a key improvement in CXCR4-targeting radioligands derived from the endogenous peptide inhibitor EPI-X4: the removal of a lysine residue in their octapeptide sequence. By reducing the radioligand's overall charge, this modification effectively lowers the undesirably high kidney accumulation seen in the first generation of these radioligands and improves CXCR4 affinity. This work brings EPI-X4 derived radiotheranostics closer to actuation. More details can be found in 10.1002/cmdc.202400773 by Melpomeni Fani and co-workers.
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Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies.
ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs.
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