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BACE1 Inhibitor Peptides: Can an Infinitely Small k(cat) Value Turn the Substrate of an Enzyme into Its Inhibitor?

[Image: see text] Recently, we reported substrate-based pentapeptidic β-secretase (BACE1) inhibitors with a hydroxymethylcarbonyl isostere as a substrate transition-state mimic. These inhibitors showed potent BACE1 inhibitory activity in enzyme and cell assays, with KMI-429 showing in vivo inhibitio...

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Bibliografske podrobnosti
Main Authors: Hamada, Yoshio, Ishiura, Shoichi, Kiso, Yoshiaki
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2011
Online dostop:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025764/
https://ncbi.nlm.nih.gov/pubmed/24900449
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml2002373
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