Muhammet Tanc, Nicolò Filippi, Yentl Van Rymenant, Sergei Grintsevich, Isabel Pintelon, Marlies Verschuuren, Joni De Loose, Emile Verhulst, Euy Sung Moon, Lorenzo Cianni, Sigrid Stroobants, Koen Augustyns, Frank Roesch, Ingrid De Meester, Filipe Elvas, Pieter Van der Veken
Fibroblast activation protein (FAP) is a very reliable biomarker for tissue remodeling. FAP has so far mainly been studied in oncology, but there is growing interest in the enzyme in other diseases like fibrosis. Recently, FAP-targeting diagnostics and therapeutics have emerged, of which the so-called FAPIs are among the most promising representatives. FAPIs typically have a relatively high molecular weight and contain very polar, multicharged chelator moieties. While this is not limiting the application of FAPIs in oncology, more druglike FAPIs could be required to optimally study diseases characterized by denser, less permeable tissue...
April 24, 2024: Journal of Medicinal Chemistry