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  • Title: Structure-based design of novel, urea-containing FKBP12 inhibitors.
    Author: Dragovich PS, Barker JE, French J, Imbacuan M, Kalish VJ, Kissinger CR, Knighton DR, Lewis CT, Moomaw EW, Parge HE, Pelletier LA, Prins TJ, Showalter RE, Tatlock JH, Tucker KD, Villafranca JE.
    Journal: J Med Chem; 1996 Apr 26; 39(9):1872-84. PubMed ID: 8627611.
    Abstract:
    The structure-based design and subsequent chemical synthesis of novel, urea-containing FKBP12 inhibitors are described. These compounds are shown to disrupt the cis-trans peptidylprolyl isomerase activity of FKBP12 with inhibition constants (Ki,app) approaching 0.10 microM. Analyses of several X-ray crystal structures of FKBP12-urea complexes demonstrate that the urea-containing inhibitors associate with FKBP12 in a manner that is similar to, but significantly different from, that observed for the natural product FK506.
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