Different chemoenzymatic strategies for the preparation of carbohydrates and analogues possessing
antidiabetic or anticancer activity are summarized. In this sense, some examples illustrating the use
of enzymes such as aldolases, lipases or glycosidases (in some cases improved by genetic engineering
techniques) are presented, showing the advantages of the implementation of chemoenzymatic protocols, which combine
the flexibility of chemical synthesis with the efficiency, selectivity and sustainability of biotransformations to obtain diverse
complex carbohydrates, glycoconjugates and glycomimetics.