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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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