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Synthesis of a C-terminally biotinylated macrocyclic peptide mimetic exhibiting high Grb2 SH2 domain-binding affinity

  1. Author:
    Shi, Z. D.
    Liu, H. P.
    Zhang, M. C.
    Worthy, K. M.
    Bindu, L.
    Yang, D. J.
    Fisher, R. J.
    Burke, T. R.

  2. Author Address

    NCI, CCR, Med Chem Lab, NIH, Frederick, MD 21702 USA. Univ Michigan, Sch Med, Ann Arbor, MI 48109 USA. SAIC Frederick, Prot Chem Lab, Frederick, MD 21702 USA Burke, TR, NCI, CCR, Med Chem Lab, NIH, Frederick, MD 21702 USA
    1. Year: 2005
    2. Date: JUL 1
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 13
    2. 13
    3. Pages: 4200-4208
  4. Type of Article: Article
  1. Abstract:

    Although considerable effort has been devoted to developing Grb2 SH2 domain-binding antagonists, important questions related to ligand specificity, and identification of intracellular targets remain unanswered. In order to begin addressing these issues, the design, synthesis, and evaluation of a novel biotinylated macrocycle are reported that bears biotin functionality at a C-terminal rather than the traditional N-terminal position. With a Grb2 SH2 domain-binding K-eq value of 3.4 nM, the title macrocycle (5) is among the most potent biotinylated SH2 domain-binding ligands yet disclosed. This should be a useful tool for elucidating physiological targets of certain Grb2 SH2 domain-binding antagonists. (c) 2005 Elsevier Ltd. All rights reserved

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External Sources

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  2. DOI: 10.1016/j.bmc.2005.04.028
  3. View record in Web of Science®
  4. WOS: 000229811900008

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