Biocatalytic Synthesis of Corticosteroid Derivatives by Toad-Derived Steroid C21-Hydroxylase

CsCYP21A, a steroid 21-hydroxylase from <i>Bufo bufo gargarizans</i>, exhibits unprecedented sequential oxidations. Optimizing <i>Pichia pastoris</i> biotransformation conditions enhanced C21-hydroxylation selectivity, converting 14 substrates to 21-hydroxylated products, with 10 conversions of >80% and 4 yields of >80%. Hydrocortisone production reached 1.5 g L<sup>-1</sup> day<sup>-1</sup> with 100 g/L wet biomass. CsCYP21A's versatility enables integration into the synthesis of over 10 steroidal drugs, offering a sustainable biocatalytic platform for green pharmaceutical manufacturing.

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Publication Details

Journal
Organic Letters
Published
2025-04-17
DOI
https://doi.org/10.1021/acs.orglett.5c00639
Citations
1
Primary Topic
Steroid Chemistry and Biochemistry
Type
article
Field-Weighted Citation Impact
0.81

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article

Biocatalytic Synthesis of Corticosteroid Derivatives by Toad-Derived Steroid C21-Hydroxylase

Xueqing Zhong, Jia-Xu Qin, Qunfei Zhao, Qingli He et al.
1 citations
Organic Letters
Steroid Chemistry and Biochemistry
0.81
article

Biocatalytic Synthesis of Corticosteroid Derivatives by Toad-Derived Steroid C21-Hydroxylase

Xueqing Zhong, Jia-Xu Qin, Qunfei Zhao, Qingli He, Mengmeng Duan, Guo‐Qiang Lin
article en
1 citations

Abstract

CsCYP21A, a steroid 21-hydroxylase from <i>Bufo bufo gargarizans</i>, exhibits unprecedented sequential oxidations. Optimizing <i>Pichia pastoris</i> biotransformation conditions enhanced C21-hydroxylation selectivity, converting 14 substrates to 21-hydroxylated products, with 10 conversions of >80% and 4 yields of >80%. Hydrocortisone production reached 1.5 g L<sup>-1</sup> day<sup>-1</sup> with 100 g/L wet biomass. CsCYP21A's versatility enables integration into the synthesis of over 10 steroidal drugs, offering a sustainable biocatalytic platform for green pharmaceutical manufacturing.

Organic LettersVol. 27(17)
Shanghai University of Traditional Chinese Medicine (CN)
Shanghai Science and Technology Development Foundation, Shanghai Municipal Health Commission, National Natural Science Foundation of China, Shanghai University of Traditional Chinese Medicine
Openalex Percentile: Top 29%
Steroid Chemistry and Biochemistry
0.81
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