ArticleAngewandte Chemie (International ed. in English)2021
High-Throughput Quality Control Assay for the Solid-Phase Synthesis of DNA-Encoded Libraries of Macrocycles*.
Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 24 citations in OpenAlex.
- Solid-Phase Synthesis of Diverse Macrocycles by Regiospecific 2-Pyridone Formation: Scope and Applications.JACS Au · 2024Article
- Encoding and display technologies for combinatorial libraries in drug discovery: The coming of age from biology to therapy.Acta pharmaceutica Sinica. B · 2024Review
- Evolution of chemistry and selection technology for DNA-encoded library.Acta pharmaceutica Sinica. B · 2024Review
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale.Nature communications · 2022Article
- Synthesis and Screening of a DNA-Encoded Library of Non-Peptidic Macrocycles.Angewandte Chemie (International ed. in English) · 2022Article
- Recent advances in DNA-encoded dynamic libraries.RSC chemical biology · 2022Review
- In-solution direct oxidative coupling for the integration of sulfur/selenium into DNA-encoded chemical libraries.Chemical science · 2022Article
- Recent Advances in Macrocyclic Drugs and Microwave-Assisted and/or Solid-Supported Synthesis of Macrocycles.Molecules (Basel, Switzerland) · 2022Review
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- Macrocyclic DNA-encoded chemical libraries: a historical perspective.RSC chemical biology · 2022Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
There is considerable interest in the development of libraries of scaffold-diverse macrocycles as a source of ligands for difficult targets, such as protein-protein interaction surfaces. A classic problem in the synthesis of high-quality macrocyclic libraries is that some linear precursors will cyclize efficiently while some will not, depending on their conformational preferences. We report here a powerful quality control method that can be employed to readily distinguish between scaffolds that do and do not cyclize efficiently during solid-phase synthesis of thioether macrocycles without the need for tedious liquid chromatography/mass spectrometry analysis. We demonstrate that this assay can be employed to identify linear impurities in a DNA-encoded library of macrocycles. We also use the method to establish a useful quality control protocol for re-synthesis of putative macrocyclic screening hits.
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Registered trials
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.