Application of high-throughput, molecular-targeted screening to anticancer drug discovery

Curr Top Med Chem. 2002 Mar;2(3):229-46. doi: 10.2174/1568026023394317.


Increasing insight into the genetics and molecular biology of cancer has resulted in the identification of an increasing number of potential molecular targets for anti-cancer drug discovery and development. These targets can be approached through exploitation of emerging structural biology, "rational" drug design, screening of chemical libraries, or a combination of these methods. In this article we discuss the application of high-throughput screening to anti-cancer drug discovery, with special reference to approaches used at the U.S. National Cancer Institute.

Publication types

  • Review

MeSH terms

  • Algorithms
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Combinatorial Chemistry Techniques / methods
  • Drug Design
  • Drug Screening Assays, Antitumor / methods*
  • Humans


  • Antineoplastic Agents