Bioorganic & Medicinal Chemistry Letters 2001-01-08

Design and synthesis of rhodamine 110 derivative and caspase-3 substrate for enzyme and cell-based fluorescent assay.

S X Cai, H Z Zhang, J Guastella, J Drewe, W Yang, E Weber

Index: Bioorg. Med. Chem. Lett. 11(1) , 39-42, (2001)

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Abstract

N-Octyloxycarbonyl-R110 (1), with enhanced cell penetration and retention properties, was prepared from rhodamine 110. The tetrapeptide substrate N-Ac-DEVD-N'-octyloxycarbonyl-R110 (3) was prepared and shown to be efficiently cleaved by human recombinant caspase-3 and by apoptotic HL-60 cells. This substrate should prove useful in cell-based assays for apoptosis inducers and inhibitors.