Convergent Solid-Phase Synthesis of Macromolecular MUC1 Models Truly Mimicking Serum Glycoprotein Biomarkers of Interstitial Lung Diseases

2016 ◽  
Vol 138 (27) ◽  
pp. 8392-8395 ◽  
Author(s):  
Naoki Ohyabu ◽  
Kiyoshi Kakiya ◽  
Yasuhiro Yokoi ◽  
Hiroshi Hinou ◽  
Shin-Ichiro Nishimura
Keyword(s):  
Lung Diseases ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Interstitial Lung Diseases ◽  
Phase Synthesis ◽  
Serum Glycoprotein

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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