References:

    (PDB ID: 3K5V) Zhang, J.; et al. Nature 2010, 463, 501.
    (PDB ID: 3GWU) Zhou, Z.; et al. Nat. Struct. Mol. Biol. 2009, 16, 652.
    (PDB ID: 3CLD) Biggadike, K.; et al. J. Med. Chem. 2008, 51, 3349.
    (PDB ID: 3L2T) Hare, S.; et al. Nature 2010, 464, 232.

Other Webpages of Interest:

    Wikipedia - Drug Design - Wikipedia offers a broad overview of the topic of logical drug design.
    Tagamet®: A medicine that changed people's lives - This article, written for the American Chemical Society's "Historic Chemical Landmarks Program" details the discovery of Tagamet® (Cimetidine), one of the first logically-designed drugs to come to market.
    Farber, G.K. Pharmacology & Therapeutics 1999, 84, 327. - This review article, although a bit dated, provides some useful visuals to illustrate key principles behind rational drug design.
    Wlodawer, A. Annu. Rev. Med. 2002, 53, 595. - Another review article. This one details the logical development of several AIDS drugs.
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