Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic

…, KJ D'Alessio, MS McQueney, J Kurdyla…

文献索引：Thompson, Scott K.; Smith, Ward W.; Zhao, Baoguang; Halbert, Stacie M.; Tomaszek, Thaddeus A.; Tew, David G.; Levy, Mark A.; Janson, Cheryl A.; D'Alessio, Karla J.; McQueney, Michael S.; Kurdyla, Jeff; Jones, Christopher S.; Desjarlais, Renee L.; Abdel-Meguid, Sherin S.; Veber, Daniel F. Journal of Medicinal Chemistry, 1998 , vol. 41, # 21 p. 3923 - 3927

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被引用次数: 26

摘要

Peptidomimetic cathepsin K inhibitors have been designed using binding models which were based on the X-ray crystal structure of an amino acid-based, active site-spanning inhibitor complexed with cathepsin K. These inhibitors, which contain a benzyloxybenzoyl group in place of a Cbz-leucine moiety, maintained good inhibitory potency relative to the amino acid-based inhibitor, and the binding models were found to be very predictive of ...