A combinatorial biocatalysis approach to an array of cholic acid derivatives

Abstract A 39‐member library of bile acid derivatives was prepared starting from 3α,7α,12α‐trihydroxy‐5β‐cholan‐24‐oic acid methyl ester using a combinatorial biocatalytic approach. A regioselective oxidation step, catalyzed by hydroxysteroid dehydrogenases, followed by an acylation step with a seri...

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Bibliographic Details
Published in:Biotechnology and Bioengineering
Main Authors: Secundo, Francesco, Carrea, Giacomo, De Amici, Marco, Joppolo di Ventimiglia, Samuele, Dordick, Jonathan S.
Format: Article in Journal/Newspaper
Language:English
Published: Wiley 2002
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Online Access:http://dx.doi.org/10.1002/bit.10486
https://onlinelibrary.wiley.com/doi/pdf/10.1002/bit.10486
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Summary:Abstract A 39‐member library of bile acid derivatives was prepared starting from 3α,7α,12α‐trihydroxy‐5β‐cholan‐24‐oic acid methyl ester using a combinatorial biocatalytic approach. A regioselective oxidation step, catalyzed by hydroxysteroid dehydrogenases, followed by an acylation step with a series of different acyl donors catalyzed by Candida antarctica lipase B, led to the modification of the bile acid scaffold. Each member of the library was obtained in high purity and good yield. © 2003 Wiley Periodicals, Inc. Biotechnol Bioeng 81: 391–396, 2003.