Solid-Phase Synthesis of a Nonpeptide RGD Mimetic Library:  New Selective αvβ3 Integrin Antagonists

2001 ◽  
Vol 44 (12) ◽  
pp. 1938-1950 ◽  
Author(s):  
Gábor A. G. Sulyok ◽  
Christoph Gibson ◽  
Simon L. Goodman ◽  
Günter Hölzemann ◽  
Matthias Wiesner ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Αvβ3 Integrin ◽  
Phase Synthesis ◽  
Integrin Antagonists

Solid-phase synthesis of dual α4β1/α4β7 integrin antagonists: two scaffolds with overlapping pharmacophores

2002 ◽  
Vol 12 (20) ◽  
pp. 2913-2917 ◽  
Author(s):  
Georgette M. Castanedo ◽  
Fredrick C. Sailes ◽  
Nathan J.P. Dubree ◽  
John B. Nicholas ◽  
Lisa Caris ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Integrin Antagonists

Solid-phase synthesis of a selective αvβ3 integrin antagonist library

1997 ◽  
Vol 7 (11) ◽  
pp. 1371-1376 ◽  
Author(s):  
Jeffrey W. Corbett ◽  
Nilsa R. Graciani ◽  
Shaker A. Mousa ◽  
William F. DeGrado
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Αvβ3 Integrin ◽  
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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