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OleD Loki as a Catalyst for Hydroxamate Glycosylation
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Published Date:
November 26 2019
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Source:Chembiochem. 21(7):952-957
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Language:English
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Details:
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Alternative Title:Chembiochem
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Personal Author:
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Description:Herein we describe the ability of the permissive glycosyltransferase (GT) OleD Loki to convert a diverse set of >15 histone deacetylase (HDAC) inhibitors (HDACis) into their corresponding hydroxamate glycosyl esters. Representative glycosyl esters were subsequently evaluated in assays for cancer cell line cytotoxicity, chemical and enzymatic stability, and axolotl embryo tail regeneration. Computational substrate docking models were predictive of enzyme-catalyzed turnover and suggest certain HDACis may form unproductive, potentially inhibitory, complexes with GTs.
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Subject:
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Pubmed ID:31621997
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Pubmed Central ID:PMC7124993
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