Details

Autor(en) / Beteiligte

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

Titel

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

Ist Teil von

• Doklady. Biochemistry and biophysics, 2016-09, Vol.470 (1), p.338-341

Ort / Verlag

Moscow: Pleiades Publishing

Erscheinungsjahr

2016

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.