Synthesis, enzymatic evaluation, and docking studies of fluorogenic caspase 8 tetrapeptide substrates

P Reszka, R Schulz, K Methling, M Lalk…

Index: Reszka, Przemyslaw; Schulz, Riad; Methling, Karen; Lalk, Michael; Bednarski, Patrick J. ChemMedChem, 2010 , vol. 5, # 1 p. 103 - 117

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Citation Number: 10

Abstract

Abstract The synthesis, enzymatic evaluation, and molecular modeling studies of new fluorogenic tetrapeptide-based substrates selective for caspase 8, having the general structure Ac-IETD–AXX, are described. Various fluorescent reporter groups (AXX), ie, 3-and 4-substituted coumarins and quinolin-2 (1H)-ones were synthesized by von Pechmann condensation. They were subsequently coupled with the caspase-8-selective tetrapeptide ...