ArticleSLAS discovery : advancing life sciences R & D2018
Robustness of In Vitro Selection Assays of DNA-Encoded Peptidomimetic Ligands to CBX7 and CBX8.
Article in SLAS discovery : advancing life sciences R & D, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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Who cites it
28 citing papers in PubMed.
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- Structural landscape of H3K27me3 recognition by protein domains and their potential for inhibition.The Journal of biological chemistry · 2026Review
- Universal Baseline forbioRxiv : the preprint server for biology · 2026Article
- A hybrid unsupervised methodology on artificial intelligence filtering for automatically processing cellular DNA-encoded library (DEL) datasets.Bioinformatics (Oxford, England) · 2026Article
- Evaluation of multiplexed liquid glycan Array (LiGA) for serological detection of glycan-binding antibodies.Glycobiology · 2025Article
- Unravelling the impact of the chromobox proteins in human cancers.Cell death & disease · 2025Review
- Epigenetic regulatory protein chromobox family regulates multiple signalling pathways and mechanisms in cancer.Clinical epigenetics · 2025Review
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Machine-Learning-Based Data Analysis Method for Cell-Based Selection of DNA-Encoded Libraries.ACS omega · 2023Article
- Chromobox proteins in cancer: Multifaceted functions and strategies for modulation (Review).International journal of oncology · 2023Review
- Machine Learning on DNA-Encoded Library Count Data Using an Uncertainty-Aware Probabilistic Loss Function.Journal of chemical information and modeling · 2022Review
- Recent advances in DNA-encoded dynamic libraries.RSC chemical biology · 2022Review
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- Discovery of Potent Peptidomimetic Antagonists for Heterochromatin Protein 1 Family Proteins.ACS omega · 2022Article
- Article
- A Potent, Selective CBX2 Chromodomain Ligand and Its Cellular Activity During Prostate Cancer Neuroendocrine Differentiation.Chembiochem : a European journal of chemical biology · 2021Article
- Scanning Protein Surfaces with DNA-Encoded Libraries.ChemMedChem · 2021Review
- The 2020SLAS discovery : advancing life sciences R & D · 2021Article
- Design and Construction of a Focused DNA-Encoded Library for Multivalent Chromatin Reader Proteins.Molecules (Basel, Switzerland) · 2020Article
- Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor.ACS chemical biology · 2020Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The identification of protein ligands from a DNA-encoded library is commonly conducted by an affinity selection assay. These assays are often not validated for robustness, raising questions about selections that fail to identify ligands and the utility of enrichment values for ranking ligand potencies. Here, we report a method for optimizing and utilizing affinity selection assays to identify potent and selective peptidic ligands to the highly related chromodomains of CBX proteins. To optimize affinity selection parameters, statistical analyses (Z' factors) were used to define the ability of selection assay conditions to identify and differentiate ligands of varying affinity. A DNA-encoded positional scanning library of peptidomimetics was constructed around a trimethyllysine-containing parent peptide, and parallel selections against the chromodomains from CBX8 and CBX7 were conducted over three protein concentrations. Relative potencies of off-DNA hit molecules were determined through a fluorescence polarization assay and were consistent with enrichments observed by DNA sequencing of the affinity selection assays. In addition, novel peptide-based ligands were discovered with increased potency and selectivity to the chromodomain of CBX8. The results indicate low DNA tag bias and show that affinity-based in vitro selection assays are sufficiently robust for both ligand discovery and determination of quantitative structure-activity relationships.
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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.