325705-48-4Relevant articles and documents
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: Peptidomimetic replacement of the P2 amino acid by 2-aminoaryl acids and other non-natural amino acids
Wang, Yan,Jia, Shaojuan,Tseng, Ben,Drewe, John,Cai, Sui Xiong
, p. 6178 - 6182 (2008/04/02)
As a continuation of our SAR studies of dipeptidyl aspartyl-fmk as caspase inhibitors, we explored the replacement of the P2 amino acid by a 2-aminoaryl acid or other non-natural amino acids. Several of these compounds, such as 6l and 6p, were
Design and synthesis of an affinity probe that targets caspases in proteomic experiments
Liau, Ming-Lee,Panicker, Resmi C.,Yao, Shao Q.
, p. 1043 - 1046 (2007/10/03)
The field of proteomics aims to study all proteins in the human proteome. This huge task may be accelerated by using active-site directed probes which profile proteins in an activity-dependent manner. Herein, we have developed a fluorescently-labeled affinity probe containing chemical reactivity specific towards caspases. Preliminary assays and proof-of-concept experiments demonstrated that this probe exhibits strong chemical reactivity towards caspase-1 over other enzymes, capable of covalently labeling caspapse-1 over other non-caspase enzymes. This thus demonstrates its selectivity and potential in high-throughput screenings of other unknown caspases in a large-scale proteomics experiment.
Dipeptide apoptosis inhibitors and the use thereof
-
, (2008/06/13)
The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Synthesis of P1 Aspartate-Based Peptide Acyloxymethyl and Fluoromethyl Ketones as Inhibitors of Interleukin-1β-Converting Enzyme
Revesz, Laszlo,Briswalter, Chantal,Heng, Richard,Leutwiler, Albert,Mueller, Rudolf,Wuethrich, Hans-Juerg
, p. 9693 - 9696 (2007/10/02)
Improved procedures have been developed for the synthesis of P1 aspartate-based 2,6-dichlorobenzoyloxymethyl ketone 1 and fluoromethyl ketone 2, the prodrugs of two potent ICE-inhibitors. 1 was prepared from (R)-trans-4,5-O-isopropylidene-4,5-dihydroxy-2-