Small targeted cytotoxics: current state and promises from DNA-encoded chemical libraries.

Nikolaus Krall, Jörg Scheuermann, Dario Neri

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, Swiss Federal Institute of Technology Zurich, Wolfgang-Pauli-Strasse 10, CH-8093 Zürich, Switzerland.

Angewandte Chemie (International ed. in English) 2013 Jan 28

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The targeted delivery of potent cytotoxic agents has emerged as a promising strategy for the treatment of cancer and other serious conditions. Traditionally, antibodies against markers of disease have been used as drug-delivery vehicles. More recently, lower molecular weight ligands have been proposed for the generation of a novel class of targeted cytotoxics with improved properties. Advances in this field crucially rely on efficient methods for the identification and optimization of organic molecules capable of high-affinity binding and selective recognition of target proteins. The advent of DNA-encoded chemical libraries allows the construction and screening of compound collections of unprecedented size. In this Review, we survey developments in the field of small ligand-based targeted cytotoxics and show how innovative library technologies will help develop the drugs of the future. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Citation

Nikolaus Krall, Jörg Scheuermann, Dario Neri. Small targeted cytotoxics: current state and promises from DNA-encoded chemical libraries. Angewandte Chemie (International ed. in English). 2013 Jan 28;52(5):1384-402