scholarly journals Tetrahydroimidazo[1,2‐ a ]pyrazine Derivatives: Synthesis and Evaluation as Gα q ‐Protein Ligands

2020 ◽  
Vol 26 (55) ◽  
pp. 12615-12623
Author(s):  
Jim Küppers ◽  
Tobias Benkel ◽  
Suvi Annala ◽  
Kenichi Kimura ◽  
Lisa Reinelt ◽  
...  
Keyword(s):  
2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek

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.


2006 ◽  
Vol 128 (7) ◽  
pp. 2160-2161 ◽  
Author(s):  
Mikhail Reibarkh ◽  
Thomas J. Malia ◽  
Gerhard Wagner

2009 ◽  
Vol 16 (26) ◽  
pp. 3359-3380 ◽  
Author(s):  
S. Taliani ◽  
F. Da Settimo ◽  
E. Da Pozzo ◽  
B. Chelli ◽  
C. Martini

2001 ◽  
Vol 12 (2) ◽  
pp. 240-250 ◽  
Author(s):  
Jean P. Wiley ◽  
Karin A. Hughes ◽  
Robert J. Kaiser ◽  
Edward A. Kesicki ◽  
Kevin P. Lund ◽  
...  

PLoS ONE ◽  
2015 ◽  
Vol 10 (8) ◽  
pp. e0133571 ◽  
Author(s):  
Anna Russo ◽  
Pasqualina Liana Scognamiglio ◽  
Rolando Pablo Hong Enriquez ◽  
Carlo Santambrogio ◽  
Rita Grandori ◽  
...  

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