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Related Experiment Videos

Early discovery drug screening using mass spectrometry.

Marshall M Siegel1

  • 1Discovery Analytical Chemistry, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. siegelm@war.wyeth.com

Current Topics in Medicinal Chemistry
|March 20, 2002
PubMed
Summary

This review covers electrospray ionization (ESI) and matrix-assisted laser desorption/ionization (MALDI) mass spectrometry for early drug discovery screening. These methods analyze non-covalent complexes, enabling efficient identification of drug candidates interacting with biomolecules.

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Area of Science:

  • Analytical Chemistry
  • Biochemistry
  • Pharmacology

Background:

  • Early drug discovery relies on efficient screening of small molecule ligands.
  • Identifying non-covalent interactions between ligands and biopolymers is crucial.
  • Mass spectrometry offers powerful tools for molecular analysis.

Purpose of the Study:

  • To review electrospray ionization (ESI) and matrix-assisted laser desorption/ionization (MALDI) mass spectrometric methods for early drug discovery.
  • To highlight the application of these techniques in studying non-covalent complexes.
  • To demonstrate high-throughput screening capabilities.

Main Methods:

  • Analysis of non-covalent complexes formed between biopolymer receptors and small molecule ligands.
  • Gas-phase analysis using ESI-MS under gentle conditions.

Related Experiment Videos

  • Condensed-phase analysis using ESI-MS with ancillary techniques (chromatography, filtration, centrifugation, electrophoresis).
  • Solid-phase screening using MALDI-MS with affinity probe tips and beads.

    • Main Results:

    • ESI-MS enables direct analysis of intact non-covalent complexes in the gas phase.
    • Condensed-phase techniques coupled with ESI-MS allow identification of small molecule ligands.
    • MALDI-MS facilitates solid-phase screening of bound ligands.
    • Both ESI and MALDI produce molecular ions, enabling high-throughput screening of mass-indexed mixtures.

    Conclusions:

    • ESI and MALDI mass spectrometry are versatile and effective for early drug discovery screening.
    • These methods efficiently analyze non-covalent interactions crucial for drug development.
    • The ability to analyze mass-indexed mixtures facilitates high-throughput screening.