cb500248r_si_001.pdf (1.16 MB)
A Chemical Strategy for the Cell-Based Detection of HDAC Activity
journal contribution
posted on 2015-12-17, 02:46 authored by Himashinie
V. K. Diyabalanage, Genevieve
C. Van de Bittner, Emily
L. Ricq, Jacob M. HookerA strategy
for activity-based enzyme detection using a novel enamide-based
chemical strategy is described. Enzymatic cleavage of an amide bond
results in the formation of an aldehyde. The interaction of this aldehyde
with proteins increases retention in cells that express the enzyme.
Proof of concept for this enamide-based strategy is demonstrated by
detecting histone deacetylase (HDAC) activity in HeLa cells. The modular
design of this strategy makes it amenable to in vitro and in vivo detection.