Finding the needle in the haystack: why high-throughput screening is good for your health

Breast Cancer Res. 2002;4(4):148-54. doi: 10.1186/bcr440. Epub 2002 Jun 10.


High-throughput screening is an essential component of the toolbox of modern technologies that improve speed and efficiency in contemporary cancer drug development. This is particularly important as we seek to exploit, for maximum therapeutic benefit, the large number of new molecular targets emerging from the Human Genome Project and cancer genomics. Screening of diverse collections of low molecular weight compounds plays a key role in providing chemical starting points for iterative optimisation by medicinal chemistry. Examples of successful drug discovery programmes based on high-throughput screening are described, and these offer potential in the treatment of breast cancer and other malignancies.

Publication types

  • Editorial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / isolation & purification
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / genetics
  • Cell Cycle / drug effects
  • Combinatorial Chemistry Techniques*
  • Drug Design*
  • Drug Evaluation, Preclinical / methods*
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology
  • Female
  • Genomics
  • Growth Inhibitors / isolation & purification
  • Growth Inhibitors / pharmacology
  • Human Genome Project
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Protein Kinase Inhibitors
  • Tumor Suppressor Protein p53 / agonists
  • Tumor Suppressor Protein p53 / antagonists & inhibitors


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Growth Inhibitors
  • Protein Kinase Inhibitors
  • Tumor Suppressor Protein p53