scholarly journals Inhibition of FAD-dependent lysine-specific demethylases by chiral polyamine analogues

RSC Advances ◽  
2018 ◽  
Vol 8 (64) ◽  
pp. 36895-36902 ◽  
Author(s):  
Naoki Umezawa ◽  
Kasumi Tsuji ◽  
Shin Sato ◽  
Masaki Kikuchi ◽  
Hisami Watanabe ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Polyamine Analogues

Polyamine-based inhibitors of lysine-specific demethylases 1 and 2 (LSD1 and LSD2) have been developed using solid-phase synthesis.

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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