How to Develop and Prove High-Efficiency Selection of Ligands from Oligonucleotide Libraries: A Universal Framework for Aptamers and DNA-Encoded Small-Molecule Ligands.

An T H Le¹, Svetlana M Krylova¹, Stanislav S Beloborodov¹, Tong Y Wang¹, Ryan Hili¹, Philip E Johnson¹, Feng Li², Rakesh N Veedu³, Svetlana Belyanskaya⁴, Sergey N Krylov¹

¹Department of Chemistry and Centre for Research on Biomolecular Interactions, York University, Toronto, Ontario M3J 1P3, Canada.

²Department of Chemistry and Centre for Biotechnology, Brock University, 1812 Sir Isaac Brock Way, St. Catharines, Ontario L2S 3A1, Canada.

³Centre for Molecular Medicine and Innovative Therapeutics, Murdoch University and Perron Institute for Neurological and Translational Science, Perth 6150, Australia.

⁴Anagenex, 10 Roessler Rd., Unit N, Woburn, Massachusetts 01801, United States.

PubMed DOI

Abstract

Screening molecular libraries for ligands capable of binding proteins is widely used for hit identification in the early drug discovery process. Oligonucleotide libraries provide a very high diversity of compounds, while the combination of the polymerase chain reaction and DNA sequencing allow the identification of ligands in low copy numbers selected from such libraries. Ligand selection from oli…

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