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Biocatalytic processes are finding increasingly widespread application not only in academia, but also in industry. This is particularly true in the pharmaceutical and agrochemical industries where the need for optically pure molecules is critical. Biocatalysis is also receiving a major thrust from the generation of new and novel biocatalysts via microbial screening, developments in the biocatalytic processes themselves (e.g. use of nonaqueous solvents for synthetic purposes) and improvements in the activation of the enzymes by numerous mechanisms (solvent and enzyme modifications), including protein engineering. The most dramatic results have been achieved by targeting the gene encoding a particular enzyme in order to undertake protein engineering by rational and non-rational methods. This review discusses various means of improving enzyme properties or creating new activities.