Evidence map›Paper›PMID 28067010›Full record

ArticleChembiochem : a European journal of chemical biology2017

Hit-Validation Methodologies for Ligands Isolated from DNA-Encoded Chemical Libraries.

Gunther Zimmermann, Yizhou Li, Ulrike Rieder, Martin Mattarella, Dario Neri, Jörg Scheuermann

Abstract read
In one paragraph

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.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Evolving a Peptide: Library Platforms and Diversification Strategies.International journal of molecular sciences · 2019
    Review
  5. Article
  6. Review
  7. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Gunther ZimmermannDepartment of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology, ETH Zürich, Vladimir-Prelog-Weg 3, 8093, Zürich, Switzerland.
Yizhou LiDepartment of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology, ETH Zürich, Vladimir-Prelog-Weg 3, 8093, Zürich, Switzerland.
Ulrike RiederPhilochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
Martin MattarellaPhilochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
Dario NeriDepartment of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology, ETH Zürich, Vladimir-Prelog-Weg 3, 8093, Zürich, Switzerland.
Jörg ScheuermannDepartment of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology, ETH Zürich, Vladimir-Prelog-Weg 3, 8093, Zürich, Switzerland.

Funding

European Research Council 670603Swiss National Science Foundation 163479
6 · The paper itself

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.

Indexed as

AcetazolamideCarbonic Anhydrase IXDNADrug DiscoveryFluorescent DyesHigh-Throughput Nucleotide SequencingLigandsNucleic Acid HybridizationOligonucleotidesProtein BindingSequence Analysis, DNASmall Molecule LibrariesAcetazolamideCarbonic Anhydrase IXDNAFluorescent DyesLigandslocked nucleic acidOligonucleotidesSmall Molecule LibrariesDNA-encoded chemical librariesdrug discoveryfluorescence anisotropyhigh-throughput screeninghit validationkoff

Identifiers

PMID28067010
PMCPMC5722192

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.