ChemInform Abstract: The 6-Hydroxy Group of Inositol 1-Phosphate Serves as an H-Bond Donor in Its Catalytic Hydrolysis by Inositol Monophosphatase: Design and Solid-Phase Synthesis of Mechanism Based Inhibitors

ChemInform ◽  
2010 ◽  
Vol 32 (51) ◽  
pp. no-no
Author(s):  
David Gani ◽  
Mahmoud Akhtar ◽  
Martin Beaton ◽  
David Miller ◽  
Roger Pybus ◽  
...  
Keyword(s):  
Hydroxy Group ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Catalytic Hydrolysis ◽  
Inositol Monophosphatase ◽  
Phase Synthesis ◽  
Inositol 1 ◽  
Synthesis Of Mechanism

Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cell Permeability ◽  
Phase Synthesis ◽  
Protein Ligands ◽  
High Affinity ◽  
Scaffold Diversity

There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.

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