Expedited Solid-Phase Synthesis of Fluorescently Labeled and Biotinylated Aminoalkane Diphenyl Phosphonate Affinity Probes for Chymotrypsin- and Elastase-Like Serine Proteases

2009 ◽  
Vol 20 (11) ◽  
pp. 2098-2105 ◽  
Author(s):  
Brendan F. Gilmore ◽  
Derek J. Quinn ◽  
Thomas Duff ◽  
George R. Cathcart ◽  
Christopher J. Scott ◽  
...  
Keyword(s):  
Serine Proteases ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Affinity Probes

scholarly journals Rapid synthesis of internal peptidyl α-ketoamides by on resin oxidation for the construction of rhomboid protease inhibitors

RSC Advances ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 4196-4199
Author(s):  
Tim Van Kersavond ◽  
Raphael Konopatzki ◽  
Merel A. T. van der Plassche ◽  
Jian Yang ◽  
Steven H. L. Verhelst
Keyword(s):  
Protease Inhibitors ◽  
Serine Proteases ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Processes ◽  
Protease Inhibition ◽  
Rapid Synthesis ◽  
Phase Synthesis ◽  
Rhomboid Protease

Rhomboid intramembrane serine proteases are involved in various biological processes. A solid phase synthesis of internal α-ketoamides reported here shows that primed site elements are crucial for rhomboid protease inhibition.

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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