title: A chemical strategy for the cell-based detection of HDAC activity.
abstract: A 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.
authors: Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School , Charlestown, Massachusetts 02129, United States.
authors: Himashinie V K
authors: HV
authors: Diyabalanage
authors: Genevieve C
authors: GC
authors: Van de Bittner
authors: Emily L
authors: EL
authors: Ricq
authors: Jacob M
authors: JM
authors: Hooker
mesh_terms: D000447:Aldehydes / Q000737:chemistry* / Q000378:metabolism; D000577:Amides / Q000737:chemistry* / Q000378:metabolism; D001681:Biological Assay / Q000379:methods*; D049109:Cell Proliferation; D002853:Chromatography, Liquid; D006367:HeLa Cells; D006655:Histone Deacetylases / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D013058:Mass Spectrometry; D018613:Microscopy, Confocal
chemical_list: D000447:Aldehydes; D000577:Amides; D006655:Histone Deacetylases