Polyarginine Peptides As a New Class of Ligands of Nicotinic Acetylcholine Receptors
- Authors: Kryukova E.V.1, Ivanov I.A.1, Lebedev D.S.1, Spirova E.N.1, Senko D.A.1, Egorova N.S.1, Kasheverov I.E.1,2, Tsetlin V.I.1
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Affiliations:
- Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
- Sechenov First Moscow State Medical University
- Issue: Vol 483, No 1 (2018)
- Pages: 313-315
- Section: Biochemistry, Biophysics, and Molecular Biology
- URL: https://journal-vniispk.ru/1607-6729/article/view/212529
- DOI: https://doi.org/10.1134/S1607672918060017
- ID: 212529
Cite item
Abstract
Arginine-containing peptides R3, R8, and R16 were obtained by solid-phase peptide synthesis, and their binding to nicotinic acetylcholine receptors (nAChRs) of muscle and neuronal (α7) types was studied by competitive radioligand assay with the use of 125I-α-bungarotoxin. The resulting peptides exhibited a significantly greater binding activity with respect to the muscle-type nAChRs than to the α7 receptor. Thus, we have discovered a new class of nAChR ligands. The affinity of the synthesized oligoarginines for nAChR depended on the number of amino acid residues in the chain. The highest affinity was exhibited by the R16 peptide, which contained 16 arginine residues.
About the authors
E. V. Kryukova
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Author for correspondence.
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
I. A. Ivanov
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
D. S. Lebedev
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
E. N. Spirova
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
D. A. Senko
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
N. S. Egorova
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
I. E. Kasheverov
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry; Sechenov First Moscow State Medical University
Email: evkr@mail.ru
Russian Federation, Moscow, 117997; Moscow, 119992
V. I. Tsetlin
Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry
Email: evkr@mail.ru
Russian Federation, Moscow, 117997
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