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Roland Weis, Richard Gaisberger, Wolfgang Skranc, Karl Gruber and Anton Glieder Carving the Active Site of Almond R-HNL for Increased Enantioselectivity Angewandte Chemie International Edition 44

Article first published online: 6 JUL 2005 | DOI: 10.1002/anie.200500435

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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.

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