Reduce HIV transmissions in Australia Appeal
Self-testing is the key to reducing undiagnosed HIV in Australia. Your support will help Professor Mark Stoové and his team make this happen.
Self-testing is the key to reducing undiagnosed HIV in Australia. Your support will help Professor Mark Stoové and his team make this happen.
The 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor MG132 that show a unique combination of high activity and selectivity for calpains over proteasome. Tripeptide aldehydes (1-3) with an aromatic P3 substituent show enhanced activity and selectivity against ovine calpain 2 relative to chymotrypsin-like activity of proteasome. Docking studies reveal the key contacts between inhibitors and calpain to confirm the importance of the S3 pocket with respect to selectivity between calpains 1 and 2 and the proteasome.
To achieve better health for vulnerable communities in Australia and internationally by accelerating the translation of research, discovery and evidence into sustainable health solutions.
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