ArticleChembiochem : a European journal of chemical biology2017
Hit-Validation Methodologies for Ligands Isolated from DNA-Encoded Chemical Libraries.
Article in Chembiochem : a European journal of chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed.
- Investigations into linker effects of DNA-VHL ligand conjugates by multiplexed affinity measurements using focal molography.RSC chemical biology · 2026Article
- DNA-Encoded Chemical Libraries: A Comprehensive Review with Succesful Stories and Future Challenges.ACS pharmacology & translational science · 2021Review
- Discovery, affinity maturation and multimerization of small molecule ligands against human tyrosinase and tyrosinase-related protein 1.RSC medicinal chemistry · 2020Article
- Evolving a Peptide: Library Platforms and Diversification Strategies.International journal of molecular sciences · 2019Review
- Application of a Substrate-Mediated Selection with c-Src Tyrosine Kinase to a DNA-Encoded Chemical Library.Molecules (Basel, Switzerland) · 2019Article
- Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.Molecules (Basel, Switzerland) · 2019Review
- DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information.Annual review of biochemistry · 2018Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
DNA-encoded chemical libraries (DECLs) are large collections of compounds linked to DNA fragments, serving as amplifiable barcodes, which can be screened on target proteins of interest. In typical DECL selections, preferential binders are identified by high-throughput DNA sequencing, by comparing their frequency before and after the affinity capture step. Hits identified in this procedure need to be confirmed, by resynthesis and by performing affinity measurements. In this article we present new methods based on hybridization of oligonucleotide conjugates with fluorescently labeled complementary oligonucleotides; these facilitate the determination of affinity constants and kinetic dissociation constants. The experimental procedures were demonstrated with acetazolamide, a binder to carbonic anhydrase IX with a dissociation constant in the nanomolar range. The detection of binding events was compatible not only with fluorescence polarization methodologies, but also with Alphascreen technology and with microscale thermophoresis.
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Registered trials
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