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Direct comparison of linear and macrocyclic compound libraries as a source of protein ligands

Academic Article
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Overview

related to degree

  • Gao, Yu (Tom), Ph.D. in Chemistry, Scripps Research , Transferred from UT Southwestern Medical Center at Dallas 2009 - 2014

authors

  • Gao, Yu (Tom)
  • Kodadek, Thomas

publication date

  • March 2015

journal

  • ACS Combinatorial Science  Journal

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.

subject areas

  • Ligands
  • Macrocyclic Compounds
  • Models, Molecular
  • Molecular Structure
  • Peptide Library
  • Peptoids
  • Small Molecule Libraries
  • Streptavidin
  • Structure-Activity Relationship
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Research

keywords

  • combinatorial library
  • high-throughput screening
  • macrocycle
  • peptoid
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Identity

PubMed Central ID

  • PMC4356041

International Standard Serial Number (ISSN)

  • 2156-8952

Digital Object Identifier (DOI)

  • 10.1021/co500161c

PubMed ID

  • 25623285
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Additional Document Info

start page

  • 190

end page

  • 195

volume

  • 17

issue

  • 3

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