Literature DB >> 31621997

OleD Loki as a Catalyst for Hydroxamate Glycosylation.

Ryan R Hughes1, Khaled A Shaaban1, Larissa V Ponomareva1, Jamie Horn1, Chunhui Zhang1, Chang-Guo Zhan1, S Randal Voss2, Markos Leggas1, Jon S Thorson1.   

Abstract

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.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  HDAC; glucosylation; glycosyltransferase; histone deacetylase

Mesh:

Substances:

Year:  2019        PMID: 31621997      PMCID: PMC7124993          DOI: 10.1002/cbic.201900601

Source DB:  PubMed          Journal:  Chembiochem        ISSN: 1439-4227            Impact factor:   3.164


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