Development of FAP-inhibitors Based on Squaric Acid Linked DOTA and DATA5m Chelators

ES Moon,F Elvas, G Vliegen,E Eppard,L Greifenstein,A Jallapally,B Klasen,V Kramer,Meester I De,S Staelens,P Van der Veken,F Rösch

Nuklearmedizin/Nuclear-Medizin（2020）

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摘要

Ziel/Aim Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts and involved in tumour–promoting processes. FAP represents an attractive target for diagnostic and therapeutic applications. In this work, new chelator-conjugates using squaric acid as linker unit based on a 4,4-difluoro substituted 2-cyanopyrrolidine FAP-inhibitor1 (UAMC1110) were synthesized and evaluated.

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