Fluorescent reporter molecules and their applications including assays for caspases

摘要

A reporter compound of formula (I), (V), or a biologically acceptable salt or pro-reporter molecule where: R1 is an N-terminal protecting group; each AA independently is a residue of an a-amino acid or b-amino acid or a derivative of an a-amino acid or b-amino acid; each n is independently is 0-5; Y is a fluorogenic or fluorescent moiety; and for formula (V) R6 is a blocking group which is not an amino acid or a derivative of an amino acid. The compounds are fluorescent dyes used in the preparation of fluorogenic or florescent peptide or amino acid derivatives which are substrates of proteases and peptidases, specifically substrates of enzymes involved in apoptosis such as caspases and the lymphocyte-derived serine protease Granzyme B. A process is also provided for measuring the activity of caspases and other enzymes involved in apoptosis in living or dead whole cells, cell lines or tissue samples derived from healthy, diseased, infected or cancerous organ tissue.