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Small Targeted Cytotoxics: Current State and Promises from DNA‐Encoded Chemical Libraries
Author(s) -
Krall Nikolaus,
Scheuermann Jörg,
Neri Dario
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201204631
Subject(s) - small molecule , computational biology , drug discovery , ligand (biochemistry) , dna , drug delivery , screening techniques , nanotechnology , biology , chemistry , computer science , microbiology and biotechnology , bioinformatics , biochemistry , materials science , receptor
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.