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Recent developments in fragment-based drug discovery.

  作者 Congreve, Miles;Chessari, Gianni;Tisi, Dominic;Woodhead, Andrew J.;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-13;  页码  3661-3680  
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[摘要]A review. The field of fragment-based drug discovery (FBDD) has developed significantly over the past 10 years and is now recognized as a tangible alternative to more traditional methods of hit identification, such as high throughput screening (HTS). The authors discuss trends and developments of FBDD over the past 4 years. Addnl., this review looks in some detail at representative protein-ligand complexes obsd. between fragment-sized mols. and their protein targets from the Protein Data Bank (PDB). More than the underlying technol. itself, the legacy of FBDD will be conceptual and that "less is more"; breaking down the problem of finding a drug mol. into its smallest component parts opens up new opportunities to solve challenging problems.

 
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