We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Rational Design of Glycomimetic Compounds Targeting the Saccharomyces cerevisiae Transglycosylase Gas2.
- Authors
Delso, Ignacio; Valero ‐ González, Jessika; Marca, Eduardo; Tejero, Tomás; Hurtado ‐ Guerrero, Ramón; Merino, Pedro
- Abstract
The transglycosylase Saccharomyces cerevisiae Gas2 ( ScGas2) belongs to a large family of enzymes that are key players in yeast cell wall remodeling. Despite its biologic importance, no studies on the synthesis of substrate-based compounds as potential inhibitors have been reported. We have synthesized a series of docking-guided glycomimetics that were evaluated by fluorescence spectroscopy and saturation-transfer difference ( STD) NMR experiments, revealing that a minimum of three glucose units linked via a β-(1,3) linkage are required for achieving molecular recognition at the binding donor site. The binding mode of our compounds is further supported by STD- NMR experiments using the active site-mutants Y107Q and Y244Q. Our results are important for both understanding of ScGas2-substrate interactions and setting up the basis for future design of glycomimetics as new antifungal agents.
- Subjects
GLYCOSYLTRANSFERASES; SACCHAROMYCES cerevisiae; PHYSIOLOGICAL effects of enzymes; FLUORESCENCE spectroscopy; MOLECULAR recognition
- Publication
Chemical Biology & Drug Design, 2016, Vol 87, Issue 2, p163
- ISSN
1747-0277
- Publication type
Editorial
- DOI
10.1111/cbdd.12650