Chemical Synthesis and Application of C-Terminally 5-Carboxyfluorescein-labelled Thymopentin as a Fluorescent Probe for Thymopoietin Receptor

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  • ONOUE Satomi
    Department of Analytical Chemistry, Faculty of Pharmaceutical Sciences, Toho University Analytical Research and Development, Pfizer Global Research and Development, Nagoya Laboratories, Pfizer Japan Inc.
  • LIU Baosheng
    American Peptide Company
  • NEMOTO Yoshitaka
    American Peptide Company
  • HIROSE Mariko
    Pharmaceutical Division, Ito Life Sciences Inc.
  • YAJIMA Takehiko
    Department of Analytical Chemistry, Faculty of Pharmaceutical Sciences, Toho University

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Description

Thymopentin (TP5) is a synthetic pentapeptide fragment, which corresponds to position 32 - 36 of thymic polypeptide thymopoietin. Thymopoietin and TP5 display a variety of biological functions, including phenotypic differentiation of T cells and the regulation of immune systems. Previous chemical modification experiments suggested that there was an absolute requirement for N-terminal amino acids to maintain the biological activity of TP5. On the basis of this structure-activity relationship, we designed and synthesized the C-terminally 5-carboxyfluorescein-coupled TP5 (TP5-FAM) as a fluorescent probe for thymopoietin receptor. TP5-FAM could bind to the membrane of human lymphoid cell lines, MOLT-4 cells, in which the thymopoietin receptor is expressed. The binding is specific and saturable (Kd = 33 µM). TP5 and human splenopentin are nearly equipotent inhibitors of TP5-FAM binding to the thymopoietin receptor, but porcine secretin did not show any significant inhibition of TP5-FAM binding to MOLT-4 cells. Thus, TP5-FAM is suggested to be a potent and biologically active ligand that would be useful for studying the binding and functional characteristics of the human thymopoietin receptor.

Journal

  • Analytical Sciences

    Analytical Sciences 22 (12), 1531-1535, 2006

    The Japan Society for Analytical Chemistry

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