Abstract
Acid sphingomyelinase (ASM) is a potential drug target and involved in rapid lipid signalling events. However, there are no tools available to adequately study such processes. Based on a non cell-permeable PtdIns(3,5)P2 inhibitor of ASM, we developed a compound with o-nitrobenzyl photocages and butyryl esters to transiently mask hydroxyl groups. This resulted in a potent light-inducible photocaged ASM inhibitor (PCAI). The first example of a time-resolved inhibition of ASM was shown in intact living cells.
Highlights
Kevin Prause,a Gita Naseri, a Fabian Schumacher, bc Christian Kappe,a Burkhard Kleuserb and Christoph Arenz *a
Based on a non cell-permeable PtdIns(3,5)P2 inhibitor of Acid sphingomyelinase (ASM), we developed a compound with o-nitrobenzyl photocages and butyryl esters to transiently mask hydroxyl groups
This resulted in a potent light-inducible photocaged ASM inhibitor (PCAI)
Summary
Kevin Prause,a Gita Naseri, a Fabian Schumacher, bc Christian Kappe,a Burkhard Kleuserb and Christoph Arenz *a. Based on a non cell-permeable PtdIns(3,5)P2 inhibitor of ASM, we developed a compound with o-nitrobenzyl photocages and butyryl esters to transiently mask hydroxyl groups.
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