Investigation into the P sub(3) Binding Domain of m-Calpain Using Photoswitchable Diazo- and Triazene-dipeptide Aldehydes: New Anticataract Agents
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 S sub(3) pocket of calpain. All compounds are potent inhibitors of m-calpain, with 8b being the most active (IC sub(50) of 35 nM)....
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| Veröffentlicht in: | Journal of medicinal chemistry 2007-06, Vol.50 (12), p.2916-2920 |
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| container_end_page | 2920 |
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| container_issue | 12 |
| container_start_page | 2916 |
| container_title | Journal of medicinal chemistry |
| container_volume | 50 |
| creator | Abell, AD Jones, MA Neffe, A T Aitken, S G Cain, T P Payne, R J McNabb, S B Coxon, J M Stuart, B G Pearson, D Lee, HY-Y Morton, J D |
| description | 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 S sub(3) pocket of calpain. All compounds are potent inhibitors of m-calpain, with 8b being the most active (IC sub(50) of 35 nM). The diazocontaining 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 (IC sub(50) of 90 nM) retards calpain-induced cataract formation in lens culture. |
| doi_str_mv | 10.1021/jm061455n |
| format | Article |
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All compounds are potent inhibitors of m-calpain, with 8b being the most active (IC sub(50) of 35 nM). The diazocontaining 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. 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| ispartof | Journal of medicinal chemistry, 2007-06, Vol.50 (12), p.2916-2920 |
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| language | eng |
| recordid | cdi_proquest_miscellaneous_19754339 |
| source | ACS Publications |
| title | Investigation into the P sub(3) Binding Domain of m-Calpain Using Photoswitchable Diazo- and Triazene-dipeptide Aldehydes: New Anticataract Agents |
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