| Autor: |
Abell AD; Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch, New Zealand. andrew.abell@canterbury.ac.nz, Jones MA, Neffe AT, Aitken SG, Cain TP, Payne RJ, McNabb SB, Coxon JM, Stuart BG, Pearson D, Lee HY, Morton JD |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2007 Jun 14; Vol. 50 (12), pp. 2916-20. Date of Electronic Publication: 2007 May 12. |
| DOI: |
10.1021/jm061455n |
| Abstrakt: |
The photoswitchable N-terminal diazo and triazene-dipeptide aldehydes 8a-d, 10a,b, and 17a,b present predominantly as the (E)-isomer, which purportedly binds deep in the S3 pocket of calpain. All compounds are potent inhibitors of m-calpain, with 8b being the most active (IC50 of 35 nM). The diazo-containing inhibitors 8a, 8c, and 10a were irradiated at 340 nm to give a photostationary state enriched in the (Z)-isomer, and in all cases, these were less active. The most water soluble triazene 17a (IC50 of 90 nM) retards calpain-induced cataract formation in lens culture. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
