European journal of medicinal chemistrySerine EndopeptidasesKineticsStructure-Activity RelationshipHumansGelatinases
In vitro kinetic profiling by enzymatic approaches to select FAPIs with a long residence time.
Emile Verhulst, Pawel Brzeminski, Anke de Groot, Joep W Wals, Robbe Michiels, Adrian Fabisiak, Jari Thys, Sergei Grintsevich, Yentl Van Rymenant, Sarah Peeters, Stijn Lambregts, Yani Sim, Ruben Verstraete, Pieter Van Wielendaele, Maya Berg
Published: 202610.1016/j.ejmech.2025.118494
Abstract
Fibroblast activation protein α (FAP) is a transmembrane serine protease overexpressed in cancer-associated fibroblasts and implicated in tumor progression and fibrosis. Although several FAP inhibitors (FAPIs) show excellent tumor uptake for positron…
Preview only. Read the full abstract at the source