ArticleACS combinatorial science2015
Direct comparison of linear and macrocyclic compound libraries as a source of protein ligands.
Article in ACS combinatorial science, 2015. 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.
- Affinity selection-mass spectrometry with linearizable macrocyclic peptide libraries.Science advances · 2025Article
- Genetically-encoded discovery of proteolytically stable bicyclic inhibitors for morphogen NODAL.Chemical science · 2021Article
- Macrocyclization of a Ligand Targeting a Toxic RNA Dramatically Improves Potency.Chembiochem : a European journal of chemical biology · 2020Article
- Direct, Competitive Comparison of Linear, Monocyclic, and Bicyclic Libraries Using mRNA Display.ACS combinatorial science · 2020Article
- Software-aided detection and structural characterization of cyclic peptide metabolites in biological matrix by high-resolution mass spectrometry.Journal of pharmaceutical analysis · 2020Article
- Protein-Catalyzed Capture Agents.Chemical reviews · 2019Review
- Chemical composition of DNA-encoded libraries, past present and future.Organic & biomolecular chemistry · 2019Review
- Peptoids advance multidisciplinary research and undergraduate education in parallel: Sequence effects on conformation and lipid interactions.Biopolymers · 2019Article
- Development of a large peptoid-DOTA combinatorial library.Biopolymers · 2016Article
- Towards vast libraries of scaffold-diverse, conformationally constrained oligomers.Chemical communications (Cambridge, England) · 2016Article
- Synthesis of a large library of macrocyclic peptides containing multiple and diverse N-alkylated residues.Molecular bioSystems · 2015Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
There has been much discussion of the potential desirability of macrocyclic molecules for the development of tool compounds and drug leads. But there is little experimental data comparing otherwise equivalent macrocyclic and linear compound libraries as a source of protein ligands. In this Letter, we probe this point in the context of peptoid libraries. Bead-displayed libraries of macrocyclic and linear peptoids containing four variable positions and 0-2 fixed residues, to vary the ring size, were screened against streptavidin and the affinity of every hit for the target was measured. The data show that macrocyclization is advantageous, but only when the ring contains 17 atoms, not 20 or 23 atoms. This technology will be useful for conducting direct comparisons between many different types of chemical libraries to determine their relative utility as a source of protein ligands.
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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.