Reaction development for DNA-encoded library technology: From evolution to revolution?

Götte, Katharina; Chines, Silvia; Brunschweiger, Andreas

doi:10.1016/j.tetlet.2020.151889

Cited by 75 publications

(71 citation statements)

References 59 publications

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“…The reactions for encoded library design have been extensively reviewed elsewhere [74,75] . DNA‐encoded compounds mirror the linear process of DNA barcode concatenation.…”

Section: Encoded Librariesmentioning

confidence: 99%

Scanning Protein Surfaces with DNA‐Encoded Libraries

et al. 2020

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Understanding the ligandability of a target protein, defined as the capability of a protein to bind drug‐like compounds on any site, can give important stimuli to drug‐development projects. For instance, inhibition of protein–protein interactions usually depends on the identification of protein surface binders. DNA‐encoded chemical libraries (DELs) allow scanning of protein surfaces with large chemical space. Encoded library selection screens uncovered several protein–protein interaction inhibitors and compounds binding to the surface of G protein‐coupled receptors (GPCRs) and kinases. The protein surface‐binding chemotypes from DELs are predominantly chemically modified and cyclized peptides, and functional small‐molecule peptidomimetics. Peptoid libraries and structural peptidomimetics have been less studied in the DEL field, hinting at hitherto less populated chemical space and suggesting alternative library designs. Roughly a third of bioactive molecules evolved from smaller, target‐focused libraries. They showcase the potential of encoded libraries to identify more potent molecules from weak, for example, fragment‐like, starting points.

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“…The reactions for encoded library design have been extensively reviewed elsewhere [74,75] . DNA‐encoded compounds mirror the linear process of DNA barcode concatenation.…”

Section: Encoded Librariesmentioning

confidence: 99%

Scanning Protein Surfaces with DNA‐Encoded Libraries

et al. 2020

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“…In the past two decades, the emergence of the DNA-encoded library (DEL) technology, also called DELT, replaced spatial encoding with DNA encoding in chemical libraries, thus overcoming the throughput limit of traditional HTS and being much more affordable and accessible to researchers. [2][3][4][5][6][7][8][9][10][11] For instance, many companies and institutions are offering DEL selection services; premade DEL kits 12 for direct use in selections and reagent kits 13 for custom DEL synthesis are also available to meet the needs of individual researchers. Furthermore, with the recent expansion of DNA-/DEL-compatible reaction toolkit, 2,6,7,[14][15][16] DELs can access much greater chemical space, which has been a major driver for its adoption in the pharmaceutical industry.…”

Section: Introduction 11 Dna-encoded Chemical Library (Del)mentioning

confidence: 99%

“…[2][3][4][5][6][7][8][9][10][11] For instance, many companies and institutions are offering DEL selection services; premade DEL kits 12 for direct use in selections and reagent kits 13 for custom DEL synthesis are also available to meet the needs of individual researchers. Furthermore, with the recent expansion of DNA-/DEL-compatible reaction toolkit, 2,6,7,[14][15][16] DELs can access much greater chemical space, which has been a major driver for its adoption in the pharmaceutical industry. 3,11,[17][18][19][20] The concept of DEL was proposed by Brenner and Lerner in 1992.…”

Section: Introduction 11 Dna-encoded Chemical Library (Del)mentioning

confidence: 99%

Recent advances in DNA-encoded dynamic libraries

Shi

Zhou

2022

RSC Chem. Biol.

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“… 10 One reason for this limitation is that the scope of chemical reactions applicable in solution-phase DEL libraries are constrained to robust reactions that preserve the integrity of the oligonucleotides; few new synthetic methodologies can be applied to DEL library construction. 11 To preserve the integrity of the DNA barcodes, chemists have continued to expand the scope of mild chemical transformations and DNA-protecting strategies (solid-phase DEL, 12 reversible absorption of DNA onto resin, 13 micellar catalyst-promoted reactions 14 ), which provides new opportunities for DEL library synthesis.…”

Section: Introductionmentioning

confidence: 99%