N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors
Authors: Jones, Seth A.; Jones, Matthew A.; McNabb, Stephen B.; Aitken, Steven G.; Coxon, James M.; Abell, Andrew D.
Source: Protein and Peptide Letters, Volume 16, Number 12, December 2009 , pp. 1466-1472(7)
Publisher: Bentham Science Publishers
Abstract:A series of Val-Leu based peptidic aldehydes containing either a furan or thiophene at the Nterminus was prepared and assayed against ovine m-calpain. In general, potency is favoured by a 2- substituted (rather than 3-substituted) heterocycle, a thiophene rather than a furan, and a shorter chain length at the N-terminus. Molecular docking experiments provide some rationale for these observations.
Document Type: Research Article
Publication date: 2009-12-01
- Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.