2024
DOI: 10.1021/acssuschemeng.4c03609
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Highly Efficient Enzymatic Synthesis of C6-Substituted Δ1-3-Ketosteroids Enabled by Finely Tuning the Substrate Binding of 3-Ketosteroid-Δ1-Dehydrogenase

Yu Wang,
Rui Zhang,
Xi Chen
et al.

Abstract: Enzymatic Δ1-dehydrogenation mediated by 3-ketosteroid-Δ1-dehydrogenases (Δ1-KstDs, EC 1.3.99.4) offers an attractive method to access pharmaceutically important Δ1-3-ketosteroids by avoiding the multistep chemical reactions and use of toxic reagents. However, Δ1-KstDs have low or no activity toward C6-substituted and other bulky 3-ketosteroids, which limits their applications in the synthesis of the corresponding dehydrogenated products that are widely used for the treatment of different diseases. Herein, str… Show more

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