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1: Nat Rev Drug Discov. 2007 Mar;6(3):211-9. Epub 2007 Feb 9.
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A decade of fragment-based drug design: strategic advances and lessons learned.

Hajduk PJ, Greer J.

Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA. philip.hajduk@abbott.com

Since the early 1990s, several technological and scientific advances - such as combinatorial chemistry, high-throughput screening and the sequencing of the human genome - have been heralded as remedies to the problems facing the pharmaceutical industry. The use of these technologies in some form is now well established at most pharmaceutical companies; however, the return on investment in terms of marketed products has not met expectations. Fragment-based drug design is another tool for drug discovery that has emerged in the past decade. Here, we describe the development and evolution of fragment-based drug design, analyse the role that this approach can have in combination with other discovery technologies and highlight the impact that fragment-based methods have made in progressing new medicines into the clinic.

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PMID: 17290284 [PubMed - indexed for MEDLINE]