ArticleFrontiers in nuclear medicine2025
Comparison of carbonic anhydrase-IX-targeted trifunctional radioligands between linear- and branched-chain arrangements.
Article in Frontiers in nuclear medicine, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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1 citing paper in PubMed.
- Development of INER-PP-F11N as the Peptide-Radionuclide Conjugate Drug Against CCK2 Receptor-Overexpressing Tumors.International journal of molecular sciences · 2025Article
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Abstract
Background: Carbonic anhydrase-IX (CA-IX) is overexpressed in tumors due to hypoxic conditions and considered an attractive biomarker for tumor-targeting radioligands. The introduction of an albumin binder (ALB) to radioligands can delay their renal clearance, resulting in increased radioactivity delivered to tumors and decreased renal uptake of radioligands. In this study, we designed novel CA-IX-targeted trifunctional radioligands consisting of imidazothiadiazole sulfonamide (IS) as a CA-IX-targeted ligand, DOTA as a chelator with four free carboxylic groups, and lysine-conjugated 4-( Methods: IS-DOTADG-ALB and DOTAGA-ALB-IS were synthesized and radiolabeled with [ Results: IS-[ Conclusion: These data suggest that the branched-chain arrangement of DOTAGA-ALB-IS may be useful for the design of CA-IX-targeted radioligands consisting of an IS ligand, DOTA, and Lys-IPBA.
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