Novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I (hDPPI)

…, C Lauritzen, G Petersen, J Pedersen, L Nærum

文献索引：Bondebjerg, Jon; Fuglsang, Henrik; Valeur, Kirsten Rosendal; Kaznelson, Dorte Wissing; Hansen, Johnny Arnsdorf; Pedersen, Rene Orup; Krogh, Berit Olsen; Jensen, Bo Skaaning; Lauritzen, Conni; Petersen, Gitte; Pedersen, John; Naerum, Lars Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 14 p. 4408 - 4424

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被引用次数: 30

摘要

Human dipeptidyl peptidase I (hDPPI, cathepsin C, EC 3.4. 14.1) is a novel putative drug target for the treatment of inflammatory diseases. Using 1 as a starting point (IC50> 10μM), we have improved potency by more than 500-fold and successfully identified novel inhibitors of DPPI via screening of a one-bead-two-compounds library of semicarbazide derivatives. Selected compounds were shown to inhibit intracellular DPPI in RBL-2H3 cells. These ...