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A Smart Library of Epoxide Hydrolase Variants and the Top Hits for Synthesis of ( S )‐β‐Blocker Precursors
Author(s) -
Kong XuDong,
Ma Qian,
Zhou Jiahai,
Zeng BuBing,
Xu JianHe
Publication year - 2014
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201402653
Subject(s) - epoxide hydrolase , epoxide , substrate (aquarium) , chemistry , epoxide hydrolase 2 , active site , enzyme , stereochemistry , combinatorial chemistry , hydrolase , biochemistry , catalysis , biology , ecology , microsome
Microtuning of the enzyme active pocket has led to a smart library of epoxide hydrolase variants with an expanded substrate spectrum covering a series of typical β‐blocker precursors. Improved activities of 6‐ to 430‐fold were achieved by redesigning the active site at two predicted hot spots. This study represents a breakthrough in protein engineering of epoxide hydrolases and resulted in enhanced activity toward bulky substrates.