Insertion of multiple α-amino γ-lactam (Agl) residues into a peptide sequence by solid-phase synthesis on synphase lanterns

Biopolymers ◽  
2010 ◽  
Vol 94 (2) ◽  
pp. 183-191 ◽  
Author(s):  
Luisa Ronga ◽  
Andrew G. Jamieson ◽  
Kim Beauregard ◽  
Christiane Quiniou ◽  
Sylvain Chemtob ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Peptide Sequence ◽  
Phase Synthesis

A convenient solid-phase synthesis methodology for preparing peptide-derived molecular imaging agents — Synthesis, characterization, and in vitro screening of Tc(I) – chemotactic peptide conjugates

2005 ◽  
Vol 83 (12) ◽  
pp. 2060-2066 ◽  
Author(s):  
Karin A Stephenson ◽  
Sangeeta Ray Banerjee ◽  
Nicole McFarlane ◽  
Douglas R Boreham ◽  
Kevin P Maresca ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Metal Chelate ◽  
Free Ligand ◽  
Peptide Sequence ◽  
In Vitro Screening ◽  
Chemotactic Peptide ◽  
Phase Synthesis ◽  
Synthesis Strategy

A versatile solid-phase synthesis strategy for preparing peptide–chelate conjugates was developed. The methodology was optimized using a series of ligands, designed to bind Tc(I)/Re(I), and a chemotactic peptide fMFL, which was exploited as a model targeting vector. The peptide derivatives were prepared in parallel using a conventional automated peptide synthesizer in multi-milligram quantities, which provided sufficient material to perform complete characterization, radiolabelling, and in vitro screening studies. Because of the robust nature of the metal–chelate complexes, the Re complex of a chelate–peptide conjugate was prepared on the resin using the same methodology employed to prepare the free ligand conjugates. As such, the reported methodology is amenable to the preparation of libraries of novel Tc radiopharmaceutical ligands and their corresponding Re reference standards in which several factors, including peptide sequence, site of derivatization, and both the type and length of the spacer, can be easily varied.Key words: radiopharmaceuticals, technetium, rhenium, peptides, 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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