N-heterocyclic dipeptide aldehyde calpain inhibitors

Date

2009

Authors

Jones, S.
Jones, M.
McNabb, S.
Aitken, S.
Coxon, J.
Abell, A.

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Protein and Peptide Letters: international journal for rapid publication of short papers in protein and peptide science, 2009; 16(12):1466-1472

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Jones, Seth A.; Jones, Matthew A.; McNabb, Stephen B.; Aitken, Steven G.; Coxon, James M. And Abell, Andrew D

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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.

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