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Πέμπτη 15 Μαρτίου 2018

Identification of NQO1 and Ferrochelatase as Interaction Partners for Neuroprotective N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides

Abstract

Affinity chromatography was used to identify potential cellular targets that are responsible for neuroprotective activity of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides. Active and inactive representatives of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides bearing an extended linker were synthesized and immobilized on an agarose based matrix. This was followed by the identification of specifically bound proteins isolated out of the whole rat brain extract. Inducible flavoprotein NAD(P)H:quinone oxidoreductase (NQO1) was identified as candidates for cellular targets.

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NQO1 was identified as a part of a nuroprotective arylpiperazine interactome. This finding points to NQO1 as a cellular target for N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-arylamides that is responsible for their neuropreotective activity.



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