Structure-activity relationship studies of a series of peptidomimetic ligands for α4β1 integrin on Jurkat T-leukemia cells

Ruiwu Liu, Li Peng, Huijun Han, Kit Lam

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

α4β1 integrin is a therapeutic target for inflammation, autoimmune diseases, and lymphoid cancers. A series of peptidomimetic ligands based on the Nle-D-I motif have been synthesized and their binding affinities (IC50) to activated α 4β1 integrin on Jurkat T-leukemia cells have been determined using a cell adhesion assay. One of the 51 ligands, 18, has been determined to have an IC50 of 0.6 nM and has a more than twofold increase of binding affinity than the initial lead compound 1. Extensive SAR studies provide important information for further ligand optimization, which has served as a foundation for studies that ultimately led to identification of a potent ligand with an IC50 of 2 pM.

Original languageEnglish (US)
Pages (from-to)595-604
Number of pages10
JournalBiopolymers - Peptide Science Section
Volume84
Issue number6
DOIs
StatePublished - 2006

Keywords

  • αβ integrin
  • Cell adhesion assay
  • Jurkat T-leukemia cells
  • Peptidomimetic ligand
  • SAR study

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Biophysics

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