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Structural Characterization of O‐ and C‐Glycosylating Variants of the Landomycin Glycosyltransferase LanGT2 |
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| Authors: | Dr Heng Keat Tam Dr Johannes Härle Dr Stefan Gerhardt Prof Dr Jürgen Rohr Guojun Wang Prof Dr Jon S Thorson Dr Aurélien Bigot Monika Lutterbeck Dr Wolfgang Seiche Prof Dr Bernhard Breit Prof Dr Andreas Bechthold Prof Dr Oliver Einsle |
| Affiliation: | 1. Institut für Biochemie, Albert‐Ludwigs‐Universit?t Freiburg, Albertstrasse 21, 79104 Freiburg (Germany);2. Institut für Pharmazeutische Wissenschaften, Albert‐Ludwigs‐Universit?t Freiburg, 79104 Freiburg (Germany);3. Center for Pharmaceutical Research and Innovation, University of Kentucky College of Pharmacy, Lexington, KY (USA);4. Institut für Organische Chemie, Albert‐Ludwigs‐Universit?t Freiburg, Albertstrasse 21, 79104 Freiburg (Germany);5. BIOSS Centre for Biological Signalling Studies, Sch?nzlestrasse 18, 79104 Freiburg (Germany) |
| Abstract: | The structures of the O‐glycosyltransferase LanGT2 and the engineered, C? C bond‐forming variant LanGT2S8Ac show how the replacement of a single loop can change the functionality of the enzyme. Crystal structures of the enzymes in complex with a nonhydrolyzable nucleotide‐sugar analogue revealed that there is a conformational transition to create the binding sites for the aglycon substrate. This induced‐fit transition was explored by molecular docking experiments with various aglycon substrates. |
| Keywords: | carbasugars C‐glycosylation enzyme engineering Friedel– Crafts alkylation glycosyltransferases |
