Fluorophosphonate-Based Degrader Identifies Degradable Serine Hydrolases by Quantitative Proteomics.

S Denise FieldWankyu LeeJason K DutraFinley Scott F SerneoJon OyerHua XuDouglas S JohnsonChristopher W Am EndeUthpala Seneviratne

Published in: Chembiochem : a European journal of chemical biology (2020)

Novel chemical biology probes linking a serine hydrolase-directed fluorophosphonate warhead and cereblon-binding pomalidomide were assessed for the degradation of serine hydrolases. A quantitative proteomics approach to detect degraded proteins revealed that, despite the engagement of ∼40 serine hydrolases, degradation was achieved for only a single serine hydrolase, lysophospholipase II (LYPLA2).

Keyphrases

protein kinase
mass spectrometry
high resolution
small molecule
genome wide
multiple myeloma
single cell
living cells
label free
binding protein
dna binding
fluorescent probe