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Higher order iminodiacetic acid libraries for probing protein-protein interactions

Academic Article
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Overview

related to degree

  • Ozer, Rachel Susan, Ph.D. in Chemistry, Scripps Research 1995 - 2001
  • Goldberg, Joel, Ph.D. in Chemistry, Scripps Research 1994 - 2000

authors

  • Boger, Dale
  • Goldberg, Joel
  • Jiang, W. Q.
  • Chai, W. Y.
  • Ducray, P.
  • Lee, Jiing-Dwan
  • Ozer, Rachel Susan
  • Andersson, C. M.

publication date

  • August 1998

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • Full details of the preparation of iminodiacetic acid diamide dimer (2040 compounds), trimer (560 compounds), and tetramer (1596 compounds) libraries by multistep convergent solution-phase synthesis for studying protein-protein interactions are provided. The libraries were assembled in a format providing small 8-10 compound mixtures and the deconvolution of many of the small mixtures to identify screening leads by resynthesis of the individual components have been conducted for 320 of the individual compounds to date. A representative example of the subsequent exploration of the structure-activity relationships for an identified receptor binding antagonist (200 additional individual compounds) and steps taken for potential elaboration to a receptor dimerization agonist are defined with preparation of representative linked dimers (70 compounds).

subject areas

  • Imides
  • Imino Acids
  • Molecular Probes
  • Polymers
  • Proteins
  • Receptors, Cytokine
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(98)00128-x

PubMed ID

  • 9784874
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Additional Document Info

start page

  • 1347

end page

  • 1378

volume

  • 6

issue

  • 8

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