Even though enzymes are the cornerstones of living systems, it has so far proven difficult to deploy artificial catalysts in a biological setting. Organocatalysts are arguably well-suited artificial catalysts for this purpose because, compared with enzymes and inorganic catalysts, they are simpler, often less toxic and widely accessible. This Review describes how organocatalysts that operate in aqueous media might enable us to selectively access new chemical transformations and provide new possibilities for chemical biology and biomedicine. Organocatalysts can be categorized according to the mechanisms by which they activate substrates, drawing comparisons with enzymes. We describe the characteristics of a catalyst that are necessary for biological compatibility and in vivo applicability, and use these to evaluate a selection of organocatalytic reactions. The attributes of the catalyst (such as functional groups and pK_a values) and the reaction (such as the microenvironment surrounding intermediates) are key considerations when developing efficient organocatalysis in aqueous media. Although we only know of a limited set of organocatalytic reactions with biological potential, on the basis of recent developments we expect a bright future for organocatalysis in biology, to the benefit of chemical biology and biomedicine.

尽管酶是生命系统的基石，但迄今为止已证明在生物环境中部署人工催化剂是困难的。有机催化剂可以说是非常适合用于此目的的人工催化剂，因为与酶和无机催化剂相比，有机催化剂更简单，通常毒性更低且易于获得。这篇综述描述了在水性介质中运行的有机催化剂如何使我们能够选择性地获得新的化学转化，并为化学生物学和生物医学提供新的可能性。可以根据它们活化底物的机制对有机催化剂进行分类，并与酶进行比较。我们描述了生物相容性和体内适用性所必需的催化剂特性，并使用它们来评估有机催化反应的选择。催化剂的属性（例如官能团和p当在水性介质中进行有效的有机催化时，K _a值）和反应（如中间体周围的微环境）是关键考虑因素。尽管我们只知道有限的一组具有生物潜力的有机催化反应，但是根据最近的发展，我们希望生物学中的有机催化有光明的未来，从而使化学生物学和生物医学受益。