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In nature, a vast number of oxidative enzymes that utilize metal ions as their active centers exist, exploiting the properties of these metal ions to oxidize substrates under mild conditions. Among these metalloenzymes, cytochrome P450 (P450) is of particular interest due to its ability to hydroxylate inert organic substrates, suggesting its potential use as a catalyst. However, P450s capable of hydroxylating the desired substrates do not always naturally exist, and often, a conversion of substrate selectivity is necessary. This article will discuss ‘how to convert the natural substrate selectivity of P450’ from a chemical perspective.

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