Medicinal chemistry of target family-directed masterkeys.
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.
Müller
Gerhard
G
Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, 81377 Münich, Germany. gerhard.mueller@axxima.com
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D015195:Drug Design; D006801:Humans