N-heterocyclic dipeptide aldehyde calpain inhibitors
Date
2009
Authors
Jones, S.
Jones, M.
McNabb, S.
Aitken, S.
Coxon, J.
Abell, A.
Editors
Advisors
Journal Title
Journal ISSN
Volume Title
Type:
Journal article
Citation
Protein and Peptide Letters: international journal for rapid publication of short papers in protein and peptide science, 2009; 16(12):1466-1472
Statement of Responsibility
Jones, Seth A.; Jones, Matthew A.; McNabb, Stephen B.; Aitken, Steven G.; Coxon, James M. And Abell, Andrew D
Conference Name
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.