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Interaction of the synthetic immunomodulatory dipeptide bestim with murine macrophages and thymocytes


The tritium-labeled dipeptide bestim (γ-D-Glu-L-Trp) with a specific activity of 45 Ci/mmol was obtained by high-temperature solid-state catalytic isotope exchange. It was found that [3H]bestim binds with a high affinity to murine peritoneal macrophages (K d 2.1 ± 0.1 nM) and thymocytes (K d 3.1 ± 0.2 nM), as well as with plasma membranes isolated from these cells (K d 18.6 ± 0.2 and 16.7 ± 0.3 nM, respectively). The specific binding of [3H]bestim to macrophages and thymocytes was inhibited by the unlabeled dipeptide thymogen (L-Glu-L-Trp) (K i 0.9 ± 0.1 and 1.1 ± 0.1 nM, respectively). After treatment with trypsin, macrophages and thymocytes lost the ability to bind [3H]bestim. Bestim in the concentration range of 10−10 to 10−6 M reduced the adenylate cyclase activity in the membranes of murine macrophages and thymocytes.

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adrenocorticotropic hormone




the glutamic acid residue that forms the peptide bond through the γ-carboxyl group


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Correspondence to E. V. Navolotskaya.

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Original Russian Text © A.A. Kolobov, N.I. Kolodkin, Yu.A. Zolotarev, C. Tuthill, E.V. Navolotskaya, 2008, published in Bioorganicheskaya Khimiya, 2008, Vol. 34, No. 1, pp. 43–49.

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Kolobov, A.A., Kolodkin, N.I., Zolotarev, Y.A. et al. Interaction of the synthetic immunomodulatory dipeptide bestim with murine macrophages and thymocytes. Russ J Bioorg Chem 34, 37–42 (2008).

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Key words

  • adenylate cyclase
  • immune system
  • peptides
  • receptors