Novel Covalent FAP-Targeted [ 68 Ga]Ga-DOTA-mFS-KERERG-FAP-2286 for Improved Pharmacokinetics and Enhanced Tumor Uptake

Molecular Pharmaceutics 2026

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Authors: Zhongcai Jin, Tongtong Wu, Shijie Tang, Yanggang Liu, Yuqi Ai, Qiang Wan, Yan Zhao, Shuang Yan, Jie Zeng, Naiguo Xing, Yang Liu, Lin Chen
+3 more Zhijun Zhou, Chen Y, Lin Qiu
DOI: 10.1021/acs.molpharmaceut.6c00249
Cited by: 1
References: 28

Abstract

Ga]Ga-DOTA-mFS-KERERG-FAP-2286 lies in its design as a derivative of the DOTA-FAP-2286 scaffold, incorporating a sulfur(VI) fluoride exchange (SuFEx)-based covalent warhead and a hydrophilic polypeptide. This modification is anticipated to alter the pharmacokinetic profile, leading to enhanced tumor uptake and retention, thereby improving clinical diagnostic accuracy.

Fields of Study & Subjects

Peptidase Inhibition and Analysis Click Chemistry and Applications Connective tissue disorders research

Publication details

Journal / source
Molecular Pharmaceutics
Publisher
American Chemical Society (ACS)
Volume
23
Issue
6
Pages
3468–3479
Publication date
29 April 2026
Language
EN