A platform for high-throughput screening of DNA-encoded catalyst libraries in organic solvents

Hook, K. Delaney; Chambers, John T.; Hili, Ryan

doi:10.1039/c7sc02779f

Cited by 31 publications

(35 citation statements)

References 35 publications

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“…The emerging OBOC‐DELs have also demonstrated the potential of DELs beyond a binding assay and suggested the possibility for phenotypic screening with DELs. We anticipate more innovations in this regard to further advance the utilities of DELs, such as selection with tissue samples, using DELs for cancer theranostics, [98] catalyst discovery, [99] and functional polymer development [100]…”

Section: Discussionmentioning

confidence: 99%

Recent Advances on the Selection Methods of DNA‐Encoded Libraries

Huang

2021

ChemBioChem

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DNA-encoded libraries (DEL) have come of age and become a major technology platform for ligand discovery in both academia and the pharmaceutical industry. Technological maturation in the past two decades and the recent explosive developments of DEL-compatible chemistries have greatly improved the chemical diversity of DELs and fueled its applications in drug discovery. A relatively less-covered aspect of DELs is the selection method. Typically, DEL selection is considered as a binding assay and the selection is conducted with purified protein targets immobilized on a matrix, and the binders are separated from the non-binding background via physical washes. However, the recent innovations in DEL selection methods have not only expanded the target scope of DELs, but also revealed the potential of the DEL technology as a powerful tool in exploring fundamental biology. In this Review, we first cover the "classic" DEL selection methods with purified proteins on solid phase, and then we discuss the strategies to realize DEL selections in solution phase. Finally, we focus on the emerging approaches for DELs to interrogate complex biological targets.

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Section: Discussionmentioning

confidence: 99%

Recent Advances on the Selection Methods of DNA‐Encoded Libraries

Huang

2021

ChemBioChem

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“…Recently, the challenge of selection against endogenous membrane proteins on live cells was overcome with the DNA‐programmed photoaffinity labeling (DPAL) approach [10] . Moreover, the keynote of DNA‐templated encoding systems has also been exploited for the discovery of novel chemical reactions [11] and catalysts [12] …”

Section: Development: Del Encoding Methods and Their Applicationsmentioning

confidence: 99%

Switchable DNA‐Encoded Chemical Library: Interconversion between Double‐ and Single‐Stranded DNA Formats

Zhao

Fan

et al. 2022

ChemBioChem

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DNA-encoded chemical libraries (DEL) have attracted substantial attention due to the infinite possibility for hit discovery in both pharmaceutical companies and academia. The encoding method is the initial step of DEL construction and one of the cornerstones of DEL applications. Classified by the DNA format, the existing DEL encoding strategies were categorized into single-stranded DNA-based strategies and double-stranded DNA-based strategies. The two DEL formats have their unique advantages but are usually incompatible with each other. To address this issue, we propose the concept of interconversion between double-and single-stranded DEL based on the "reversible covalent headpiece (RCHP)" design, which combines maximum robustness of synthesis with extraordinary flexibility of applications in distinct setups. Future opportunities in this field are also proposed to advance DEL technology to a comprehensive drug discovery platform.

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“…However, if substrates are present at high concentrations, nonlinear effects 21 may originate in such mixtures due to the cross-reactivity between multiple substrates and products. Genetically-encoded (GE) peptide libraries 9,16 and DNA-encoded small molecule libraries (DEL) [22][23][24][25][26] associate the DNA message with each substrate, and this message can be amplied from a single copy number. This amplication makes it possible to perform screening at very low concentrations of substrates.…”

Section: Introductionmentioning

confidence: 99%

Learning the structure–activity relationship (SAR) of the Wittig reaction from genetically-encoded substrates

et al. 2021

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A platform for high-throughput screening of DNA-encoded catalyst libraries in organic solvents

Abstract: PEGylation of DNA-encoded libraries enables high-throughput screening of small-molecule catalysts in organic solvents.

Cited by 31 publications

References 35 publications

Recent Advances on the Selection Methods of DNA‐Encoded Libraries

Recent Advances on the Selection Methods of DNA‐Encoded Libraries

Switchable DNA‐Encoded Chemical Library: Interconversion between Double‐ and Single‐Stranded DNA Formats

Learning the structure–activity relationship (SAR) of the Wittig reaction from genetically-encoded substrates

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