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…

Index: Jansen, Koen; Heirbaut, Leen; Verkerk, Robert; Cheng, Jonathan D.; Joossens, Jurgen; Cos, Paul; Maes, Louis; Lambeir, Anne-Marie; De Meester, Ingrid; Augustyns, Koen; Van Der Veken, Pieter Journal of Medicinal Chemistry, 2014 , vol. 57, # 7 p. 3053 - 3074

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Citation Number: 18

Abstract

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 ...

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