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https://hdl.handle.net/2440/58623
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Type: | Journal article |
Title: | N-heterocyclic dipeptide aldehyde calpain inhibitors |
Author: | Jones, S. Jones, M. McNabb, S. Aitken, S. Coxon, J. Abell, A. |
Citation: | Protein and Peptide Letters: international journal for rapid publication of short papers in protein and peptide science, 2009; 16(12):1466-1472 |
Publisher: | Bentham Science Publ Ltd |
Issue Date: | 2009 |
ISSN: | 0929-8665 1875-5305 |
Statement of Responsibility: | Jones, Seth A.; Jones, Matthew A.; McNabb, Stephen B.; Aitken, Steven G.; Coxon, James M. And Abell, Andrew D |
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. |
Keywords: | Calpain inhibitors peptidic aldehydes synthesis heterocycles |
DOI: | 10.2174/092986609789839296 |
Grant ID: | ARC |
Published version: | http://dx.doi.org/10.2174/092986609789839296 |
Appears in Collections: | Aurora harvest 5 Chemistry and Physics publications |
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