Medicinal chemistry of target family-directed masterkeys

Drug Discov Today. 2003 Aug 1;8(15):681-91. doi: 10.1016/s1359-6446(03)02781-8.


The majority of pharmaceutically relevant drug targets cluster into densely populated target families, thus offering a novel approach that complements the currently favoured screening paradigm in medicinal chemistry. This approach uses a privileged structure concept whereby molecular masterkeys are developed that account for a target family wide structural or functional commonality. Numerous lead compounds, based on multipurpose privileged structures, can be generated that address a variety of targets from a gene family of interest, irrespective of therapeutic area. Several different interpretations of the privileged structure concept will be highlighted, with a strong emphasis on the most stringent application: the optimization of a molecular masterkey for a distinct target family of interest.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Delivery Systems / methods*
  • Drug Design*
  • Humans