A Small-Molecule FRET Probe To Monitor Phospholipase A2 Activity in Cells and Organisms

2006 ◽  
Vol 45 (3) ◽  
pp. 508-512 ◽  
Author(s):  
Oliver Wichmann ◽  
Jochen Wittbrodt ◽  
Carsten Schultz
Keyword(s):  
Phospholipase A2 ◽  
Small Molecule ◽  
Phospholipase A2 Activity ◽  
In Cells

Study of phospholipase A2 activity in umbilical endothelial cells in toxemia of pregnancy.

1987 ◽  
Vol 18 (6) ◽  
pp. 582-588
Author(s):  
Hiroyuki SEKI ◽  
Toshiharu JIMBO ◽  
Kazuo SATOH
Keyword(s):  
Endothelial Cells ◽  
Phospholipase A2 ◽  
Phospholipase A2 Activity

Inhibition of NGLY1 inactivates the transcription factor Nrf1 and potentiates proteasome inhibitor cytotoxicity

2017 ◽  
Author(s):  
Carolyn Bertozzi ◽  
Fred Tomlin ◽  
Ulla Gerling-Driessen ◽  
Yi-Chang Liu ◽  
Ryan Flynn ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Small Molecule ◽  
Proteasome Inhibitor ◽  
Activation Mechanism ◽  
Cancer Drugs ◽  
Small Molecule Library ◽  
Library Screen ◽  
In Cells

We discovered that the proteostasis modulating transcription factor Nrf1 requires cytosolic de-N-glycosylation by the N-glycanase NGly1 as part of its activation mechanism. Through a covalent small molecule library screen, we discovered an inhibitor of NGly1 that blocks Nrf1 activation in cells and potentiates the activity of proteasome inhibitor cancer drugs. The requirement of NGly1 for Nrf1 activity likely underlies several pathologies associated with a rare hereditary deficiency in NGly1.

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