Synthesis and screening of bead-displayed combinatorial libraries

Todd M. Doran, Paige Dickson, John Maina Ndungu, Peng Ge, Irena Suponitsky-Kroyter, Hongchan An, Thomas Kodadek

Research output: Chapter in Book/Report/Conference proceedingChapter

6 Scopus citations


The development of faster and less expensive methods to discover bioactive small molecules remains a high priority in chemical biology. This article discusses one alternative to traditional high-throughput screening: the synthesis and screening of one bead one compound (OBOC) libraries. Protocols are provided to create and screen libraries of peptoid displayed on TentaGel beads, which is a cheap and relatively straightforward process for the identification of selective protein ligands. However, peptoids bind to proteins with modest affinity in most cases. Therefore, we also describe protocols to create libraries of stiffer oligomers called PICCOs (peptoid-inspired, conformationally constrained oligomers) that have proven to be a superior source of high affinity ligands.

Original languageEnglish (US)
Title of host publicationChemical and Synthetic Biology Approaches To Understand Cellular Functions - Part B
EditorsArun K. Shukla
PublisherAcademic Press Inc.
Number of pages37
ISBN (Print)9780128181195
StatePublished - 2019

Publication series

NameMethods in enzymology
PublisherAcademic Press Inc.
ISSN (Print)0076-6879

Bibliographical note

Funding Information:
The National Institutes of Health (AG 054892) supported some of the work described here.

Publisher Copyright:
© 2019 Elsevier Inc.


  • High-throughput screening
  • One bead one compound libraries
  • Peptoid
  • Solid-phase synthesis


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