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Bioconjug Chem. 2003 Mar-Apr;14(2):458-63.

N-Ac-DEVD-N'-(Polyfluorobenzoyl)-R110: novel cell-permeable fluorogenic caspase substrates for the detection of caspase activity and apoptosis.

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1
Maxim Pharmaceuticals, 6650 Nancy Ridge Drive, San Diego, California 92121, USA.

Abstract

N-Pentafluorobenzoyl-R110 (1a) and N-(2,3,4,5-tetrafluorobenzoyl)-R110 (1b) with enhanced cell retention properties, were prepared from rhodamine 110 (R-110) and the corresponding polyfluorobenzoyl chloride. N-Ac-DEVD-N'-pentafluorobenzoyl-R110 (3a) and N-Ac-DEVD-N'-(2,3,4,5-tetrafluorobenzoyl)-R110 (3b) were prepared as tetrapeptide substrates for caspases. Substrate 3b was efficiently cleaved by human recombinant caspase-3 in an enzyme assay. Substrate 3b also was efficiently cleaved in cell-based apoptosis assays. After cleavage in apoptotic cells by activated caspases, the substrate becomes fluorescent as measured by flow cytometry. These substrates should prove useful in cell-based assays for studying apoptosis inducers and inhibitors.

PMID:
12643757
DOI:
10.1021/bc0256188
[Indexed for MEDLINE]
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