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Macrocyclization in the design of a conformationally constrained Grb2 SH2 domain inhibitor

  1. Author:
    Gao, Y.
    Voigt, J.
    Wu, J. X.
    Yang, D. J.
    Burke, T. R.

  2. Author Address

    NCI, Frederick Canc Res & Dev Ctr, Med Chem Lab, NIH, Frederick, MD 21702 USA. NCI, Frederick Canc Res & Dev Ctr, Med Chem Lab, NIH, Frederick, MD 21702 USA. Georgetown Univ, Med Ctr, Lombardi Canc Ctr, Washington, DC 20007 USA. Burke TR NCI, Frederick Canc Res & Dev Ctr, Med Chem Lab, NIH, Frederick, MD 21702 USA.
    1. Year: 2001
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 11
    2. 14
    3. Pages: 1889-1892
  4. Type of Article: Article
  1. Abstract:

    Grubbs' olefin metathesis reaction was utilized to prepare a macrocyclic variant of a linear Grb7 SH2 domain antagonist in an attempt to induce a beta -bend conformation known to be required for high affinity binding. In extracellular Grb2 SH2 domain binding assays, the macrocyclic analogue exhibited an approximate 100-fold enhancement in binding potency relative to its linear counterpart. The macrocycle was not as effective in whole cell binding assays as would be expected based on its extracellular binding potency. (C) 2001 Elsevier Science Ltd. All rights reserved.

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