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PNA-Based Dynamic Combinatorial Libraries (PDCL) and screening of lectins.

Abstract：

:Selections from dynamic combinatorial libraries (DCL) benefit from the dynamic nature of the library that can change constitution upon addition of a selection pressure, such as ligands binding to a protein. This technology has been predominantly used with small molecules interacting with each other through reversible covalent interaction. However, application of this technology in biomedical research and drug discovery has been limited by the reversibility of covalent exchange and the analytical deconvolution of small molecule fragments. Here we report a supramolecular approach based on the use of a constant short PNA tag to direct the combinatorial pairing of fragment. This PNA tag yields fast exchange kinetics, while still delivering the benefits of cooperativity, and provides favourable properties for analytical deconvolution by MALDI. A selection from >6,000 assemblies of glycans (mono-, di-, tri-saccharides) targeting AFL, a lectin from pathogenic fungus, yielded a 95 nM assembly, nearly three orders of magnitude better in affinity than the corresponding glycan alone (41 µM).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Farrera-Soler L,Daguer JP,Raunft P,Barluenga S,Imberty A,Winssinger N

doi

10.1016/j.bmc.2020.115458

subject

Has Abstract

pub_date

2020-05-15 00:00:00

pages

115458

issue

10

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(20)30272-8

journal_volume

28

pub_type

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