Comparison of carbonic anhydrase-IX-targeted trifunctional radioligands between linear- and branched-chain arrangements.

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-(p-iodophenyl)butyric acid (Lys-IPBA) as ALB, with IS-[¹¹¹In]In-DOTADG-ALB in a linear-chain arrangement and [¹¹¹In]In-DOTAGA-ALB-IS in a branched-chain arrangement. Fundam

SUBMITTER: Nakashima K 

PROVIDER: S-EPMC12040898 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature