Labeling single domain antibody fragments with ¹⁸F using a novel residualizing prosthetic agent - N-succinimidyl 3-(1-(2-(2-(2-(2-[¹⁸F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate.

ABSTRACT:

Introduction

Labeling single domain antibody fragments (sdAbs) with ¹⁸F is an attractive strategy for immunoPET. Earlier, we developed a residualizing label, N-succinimidyl 3-((4-(4-fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([¹⁸F]RL-I), synthesized via a click reaction for labeling sdAbs with ¹⁸F, that has attractive features but suffered from modest radiochemical yields and suboptimal hydrophobicity. Herein, we have evaluated the potential utility of an analogous agent, N-succinimidyl 3-(1-(2-(2-(2-(2-[¹⁸F]fluoroethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)-5-(guanidinomethyl)benzoate ([¹⁸F]SFETGMB; [¹⁸F]RL-III) designed to address these limitations.

Methods

[¹⁸F]R

SUBMITTER: Zhou Z 

PROVIDER: S-EPMC8448961 | biostudies-literature | 2021 Sep-Oct

REPOSITORIES: biostudies-literature