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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 |