Extended Structure–Activity Relationship and Pharmacokinetic Investigation of (4-Quinolinoyl) glycyl-2-cyanopyrrolidine Inhibitors of Fibroblast Activation Protein (FAP …
…, AM Lambeir, I De Meester, K Augustyns…
文献索引：Jansen, Koen; Heirbaut, Leen; Cheng, Jonathan D.; Joossens, Jurgen; Ryabtsova, Oxana; Cos, Paul; Maes, Louis; Lambeir, Anne-Marie; De Meester, Ingrid; Augustyns, Koen; Van Der Veken, Pieter ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 5 p. 491 - 496
Fibroblast activation protein (FAP) is a serine protease related to dipeptidyl peptidase IV (DPPIV). It has been convincingly linked to multiple disease states involving remodeling of the extracellular matrix. FAP inhibition is investigated as a therapeutic option for several of these diseases, with most attention so far devoted to oncology applications. We previously discovered the N-4-quinolinoyl-Gly-(2 S)-cyanoPro scaffold as a possible entry to highly ...
