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Keywords:

  • ACE inhibitors;
  • asymmetric synthesis;
  • biocatalysis;
  • hydroxynitrile lyase;
  • protein engineering
Thumbnail image of graphical abstract

Structure-guided redesign of the active site of almond (R)-PaHNL5 for increased enantioselectivity resulted in four improved muteins. In particular, mutation V360I gave enhanced conversion rates and enantioselectivities higher than 96 % ee for two structurally related substrates 1 and 2. Chiral building blocks for the synthesis of pharmaceutically active “prils” (example shown) can thus be produced on a large scale.