Switching glycosyltransferase UGTBL1 regioselectivity toward polydatin synthesis using a semi-rational design

Bo Fan; Wenxin Dong; Tianyi Chen; Jianlin Chu; Bingfang He

doi:10.1039/c8ob00376a

Switching glycosyltransferase UGT_BL1 regioselectivity toward polydatin synthesis using a semi-rational design

Bo Fan, Wenxin Dong, Tianyi Chen, Jianlin Chu, Bingfang He

School of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

Abstract

The 62nd residue of glycosyltransferase UGT_BL1 was identified as a "hotspot" for glycosylation at 3-OH of resveratrol. Via semi-rational design including structure-guided alanine scanning and saturation mutations, the mutation I62G significantly switched the regioselectivity from 4′-OH to 3-OH of resveratrol and mainly produced polydatin (87.7%), a therapeutic natural product.

Original language	English
Pages (from-to)	2464-2469
Number of pages	6
Journal	Organic and Biomolecular Chemistry
Volume	16
Issue number	14
DOIs	https://doi.org/10.1039/c8ob00376a
State	Published - 2018

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abstract = "The 62nd residue of glycosyltransferase UGTBL1 was identified as a {"}hotspot{"} for glycosylation at 3-OH of resveratrol. Via semi-rational design including structure-guided alanine scanning and saturation mutations, the mutation I62G significantly switched the regioselectivity from 4′-OH to 3-OH of resveratrol and mainly produced polydatin (87.7%), a therapeutic natural product.",

author = "Bo Fan and Wenxin Dong and Tianyi Chen and Jianlin Chu and Bingfang He",

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AU - Fan, Bo

AU - Dong, Wenxin

AU - Chen, Tianyi

AU - Chu, Jianlin

AU - He, Bingfang

N1 - Publisher Copyright: © The Royal Society of Chemistry 2018.

PY - 2018

Y1 - 2018

N2 - The 62nd residue of glycosyltransferase UGTBL1 was identified as a "hotspot" for glycosylation at 3-OH of resveratrol. Via semi-rational design including structure-guided alanine scanning and saturation mutations, the mutation I62G significantly switched the regioselectivity from 4′-OH to 3-OH of resveratrol and mainly produced polydatin (87.7%), a therapeutic natural product.

AB - The 62nd residue of glycosyltransferase UGTBL1 was identified as a "hotspot" for glycosylation at 3-OH of resveratrol. Via semi-rational design including structure-guided alanine scanning and saturation mutations, the mutation I62G significantly switched the regioselectivity from 4′-OH to 3-OH of resveratrol and mainly produced polydatin (87.7%), a therapeutic natural product.

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U2 - 10.1039/c8ob00376a

DO - 10.1039/c8ob00376a

M3 - 文章

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AN - SCOPUS:85044991408

SN - 1477-0520

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JO - Organic and Biomolecular Chemistry

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ER -

Switching glycosyltransferase UGT_BL1 regioselectivity toward polydatin synthesis using a semi-rational design

Abstract

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