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Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain

By a process involving initial screening of a set of 87 aldehydes using an oxime ligation-based strategy, we were able to achieve a several-fold affinity enhancement over one of the most potent previously known polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors. This improved binding...

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Pubblicato in:Bioorg Med Chem Lett
Autori principali: Zhao, Xue Zhi, Hymel, David, Burke, Terrence R.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5061138/
https://ncbi.nlm.nih.gov/pubmed/27624074
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.08.098
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