Cover Feature: Improving Affinity while Reducing Kidney Uptake of CXCR4‐Targeting Radioligands Derived from the Endogenous Antagonist EPI‐X4 (ChemMedChem 6/2025)
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.
Authors
- Mirja Harms (ORCID: https://orcid.org/0000-0002-5460-5166)
- Raghuvir H. Gaonkar (ORCID: https://orcid.org/0000-0002-9097-7098)
- Thibaud Bailly (ORCID: https://orcid.org/0000-0003-4927-0522)
- Melpomeni Fani (ORCID: https://orcid.org/0000-0002-9309-1604)
- Rosalba Mansi (ORCID: https://orcid.org/0000-0003-0342-8865)
- Jacopo Millul (ORCID: https://orcid.org/0000-0003-4288-1283)
- Jan Münch (ORCID: https://orcid.org/0000-0001-7316-7141)
Institutions
- University Hospital of Basel (CH)
- Hospital Base (CL)
Publication Details
- Journal
- ChemMedChem
- Published
- 2025-03-15
- DOI
- https://doi.org/10.1002/cmdc.202580604
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00