A simple, no-wash cell adhesion-based high-throughput assay for the discovery of small-molecule regulators of the integrin CD11b/CD18

Jun Y. Park, M. Amin Arnaout, Vineet Gupta

Research output: Contribution to journalArticlepeer-review

Abstract

The leukocyte-specific integrin CD11b/CD18 plays a key role in the biological function of these cells and represents a validated therapeutic target for inflammatory diseases. Currently, the low affinity interaction between CD11b/CD18 integrin and its respective ligand poses a challenge in the development of cell-based adhesion assays for the high-throughput screening (HTS) environment. Here the authors describe a simple cell-based adhesion assay that can be readily used for HTS for the discovery of functional regulators of CD11b/CD18. The assay consistently produces acceptable Z' values (> 0.5) for HTS. After testing the assay using 2 established blocking antibodies as reference biologicals, the authors performed a proof-of-concept primary screen using a library of 6612 compounds and identified both agonist and antagonist hits.

Original languageEnglish (US)
Pages (from-to)406-417
Number of pages12
JournalJournal of Biomolecular Screening
Volume12
Issue number3
DOIs
StatePublished - Apr 2007
Externally publishedYes

Keywords

  • Cell adhesion assay
  • Integrin
  • No-wash assay
  • Primary screen

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biotechnology
  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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