scholarly journals Enhancing glycan stability via site-selective fluorination: modulating substrate orientation by molecular design

2021 ◽  
Author(s):  
Alexander Axer ◽  
Ravindra P. Jumde ◽  
Sebastian Adam ◽  
Andreas Faust ◽  
Michael Schäfers ◽  
...  
Keyword(s):  
Natural Compound ◽  
Molecular Design ◽  
Hydrolytic Stability ◽  
Single Site ◽  
Substrate Orientation ◽  
Site Selective

Single site OH → F substitution at the termini of maltotetraose leads to significantly improved hydrolytic stability towards α-amylase and α-glucosidase relative to the natural compound.

scholarly journals Enhancing Glycan Stability via Site-Selective Fluorination: Modulating Substrate Orientation by Molecular Design.

2020 ◽  
Author(s):  
Alexander Axer ◽  
Ravindra P. Jumde ◽  
Sebastian Adam ◽  
Andreas Faust ◽  
Michael Schäfers ◽  
...  
Keyword(s):  
Clinical Evaluation ◽  
Natural Compound ◽  
Molecular Design ◽  
Hydrolytic Stability ◽  
Point Mutations ◽  
Enzymatic Cleavage ◽  
Substrate Orientation ◽  
Non Invasive ◽  
Site Selective ◽  
Alpha Glucosidase

Single site OH to F substitution at the termini of maltotetraose leads to significantly improved hydrolytic stability towards alpha-amylase and alpha-glucosidase relative to the natural compound. Stability enhancements of around 1 order of magnitide result from these subtle point mutations. In both scenarios, modification of the monosaccharide furthest from the site of enzymatic cleavage leads to the greatest improvement in stability, and the configuration of the fluorine-bearing stereocenter has a clear impact on catalysis. This pre-clinical evaluation provides valuable guidelines for the development of tracer candidates for non-invasive bacterial imaging. <br>

scholarly journals Enhancing Glycan Stability via Site-Selective Fluorination: Modulating Substrate Orientation by Molecular Design.

2020 ◽  
Author(s):  
Alexander Axer ◽  
Ravindra P. Jumde ◽  
Sebastian Adam ◽  
Andreas Faust ◽  
Michael Schäfers ◽  
...  
Keyword(s):  
Clinical Evaluation ◽  
Natural Compound ◽  
Molecular Design ◽  
Hydrolytic Stability ◽  
Point Mutations ◽  
Enzymatic Cleavage ◽  
Substrate Orientation ◽  
Non Invasive ◽  
Site Selective ◽  
Alpha Glucosidase

Single site OH to F substitution at the termini of maltotetraose leads to significantly improved hydrolytic stability towards alpha-amylase and alpha-glucosidase relative to the natural compound. Stability enhancements of around 1 order of magnitide result from these subtle point mutations. In both scenarios, modification of the monosaccharide furthest from the site of enzymatic cleavage leads to the greatest improvement in stability, and the configuration of the fluorine-bearing stereocenter has a clear impact on catalysis. This pre-clinical evaluation provides valuable guidelines for the development of tracer candidates for non-invasive bacterial imaging. <br>

Single-Site Labeling of Native Proteins Enabled by a Chemoselective and Site-Selective Chemical Technology

2018 ◽  
Vol 140 (44) ◽  
pp. 15114-15123 ◽  
Author(s):  
Srinivasa Rao Adusumalli ◽  
Dattatraya Gautam Rawale ◽  
Usha Singh ◽  
Prabhanshu Tripathi ◽  
Rajesh Paul ◽  
...  
Keyword(s):  
Chemical Technology ◽  
Single Site ◽  
Native Proteins ◽  
Selective Chemical ◽  
Site Selective

Chemoselective and Site‐Selective Lysine‐Directed Lysine Modification Enables Single‐Site Labeling of Native Proteins

2020 ◽  
Vol 59 (26) ◽  
pp. 10332-10336 ◽  
Author(s):  
Srinivasa Rao Adusumalli ◽  
Dattatraya Gautam Rawale ◽  
Kalyani Thakur ◽  
Landa Purushottam ◽  
Neelesh C. Reddy ◽  
...  
Keyword(s):  
Single Site ◽  
Native Proteins ◽  
Lysine Modification ◽  
Site Selective

Chemoselective and Site‐Selective Lysine‐Directed Lysine Modification Enables Single‐Site Labeling of Native Proteins

2020 ◽  
Vol 132 (26) ◽  
pp. 10418-10422 ◽  
Author(s):  
Srinivasa Rao Adusumalli ◽  
Dattatraya Gautam Rawale ◽  
Kalyani Thakur ◽  
Landa Purushottam ◽  
Neelesh C. Reddy ◽  
...  
Keyword(s):  
Single Site ◽  
Native Proteins ◽  
Lysine Modification ◽  
Site Selective
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