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Analysis of binding centers in nicotinic receptors with the aid of synthetic peptides

  • Biochemistry, Biophysics, and Molecular Biology
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Abstract

We studies the receptor-binding specificity of the synthetic peptide HAP (High Affinity Peptide) and its analogues, which are regarded as a model of the orthosteric site nicotinic acetylcholine receptors (nAChR). Using radioligand analysis, electrophysiology tests, and calcium imaging, we assessed the ability of HAP to interact with nAChR antagonists: long α-neurotoxins and α-conotoxins. A high affinity of HAP for α-bungarotoxin and the absence of its interaction with α-cobratoxin and α-conotoxins was found. The synthesized analogues of HAP in general retained the properties of the original peptide. Thus, HAP cannot be a model of a ligand-binding site.

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Authors and Affiliations

  1. Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow, 117997, Russia

    I. E. Kasheverov, E. V. Kryukova, D. S. Kudryavtsev, I. A. Ivanov, N. V. Egorova, M. N. Zhmak, E. N. Spirova, I. V. Shelukhina & V. I. Tsetlin

  2. Photochemistry Center, Russian Academy of Sciences, ul. Novatorov 7a, Moscow, 119421, Russia

    A. V. Odinokov & M. V. Alfimov

Authors
  1. I. E. Kasheverov
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  2. E. V. Kryukova
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  3. D. S. Kudryavtsev
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  4. I. A. Ivanov
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  5. N. V. Egorova
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  6. M. N. Zhmak
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  7. E. N. Spirova
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  8. I. V. Shelukhina
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  9. A. V. Odinokov
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  10. M. V. Alfimov
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  11. V. I. Tsetlin
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Corresponding author

Correspondence to E. V. Kryukova.

Additional information

Original Russian Text © I.E. Kasheverov, E.V. Kryukova, D.S. Kudryavtsev, I.A. Ivanov, N.V. Egorova, M.N. Zhmak, E.N. Spirova, I.V. Shelukhina, A.V. Odinokov, M.V. Alfimov, V.I. Tsetlin, 2016, published in Doklady Akademii Nauk, 2016, Vol. 470, No. 3, pp. 353–356.

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Kasheverov, I.E., Kryukova, E.V., Kudryavtsev, D.S. et al. Analysis of binding centers in nicotinic receptors with the aid of synthetic peptides. Dokl Biochem Biophys 470, 338–341 (2016). https://doi.org/10.1134/S1607672916050070

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  • DOI: https://doi.org/10.1134/S1607672916050070

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