Selective Caspase Inhibitors
作者： Matthew Bogyo , Alicia B. Berger
DOI:
关键词: Legumain 、 Amino acid 、 Biology 、 Caspase 、 Recombinant DNA 、 Combinatorial chemistry 、 Caspase inhibitors 、 Highly selective 、 Covalent bond 、 Peptide 、 Biochemistry
摘要: Described here are novel, highly selective inhibitors and activity based probes (ABPs) for caspases 3, 7, 8, 9 legumain. The compounds selectively inhibit only certain caspases. A positional scanning combinatorial library (PSCL) approach was used to screen pools of peptide acyloxymethyl ketones (AOMKs) containing both natural non-natural amino acids against a number purified recombinant These screens were identify structural elements at multiple positions on the scaffold that could be modulated control inhibitor specificity towards target Further disclosed individual optimized covalent also equipped with various tags use as probes, well labeled substrates.
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