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Fiziologichnyi Zhurnal - <a id="lj1_ret_bk_to_jl0_href_id" href="?list0=18">Fiziol. Zh. 2016;</a> <a id="lj1_ret_bk_to_jl0_href_id" href="?list1=96">62(5):</a> 19-26
Українська Русский English

ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2016; 62(5): 19-26


AMINOACID RESIDUES INVOLVED IN POSITIVE MODULATION OF a1 GLYCINE RECEPTORS BY GINKGOLIC ACID

G. Maleeva1,2, S. Buldakova1, G. Skibo2, P. Bregestovski1

  1. Institute de Neurosciences des Systemes, INSERM UMR 1106, Aix-Marseille Université, France ;
  2. Bogomoletz Institute of Physiology, NAS of Ukraine, Kyiv
DOI: https://doi.org/10.15407/fz62.05.019

Abstract

Previously, we have shown that ginkgolic acid has an ability to potentiate currents, mediated by α1 subunits of glycine receptor. In order to define the mechanism of subunit specific action of ginkgolic acid we have performed comparative analysis of the amino acid sequences of α1 and α2 subunits of glycine receptor. Amino acids that contribute to the different action of ginkgolic acid on glycine receptors formed by these subunits were determined. Using whole-cell configuration of patch-clamp recording, we have demonstrated that mutation of three residues in α2 subunit for corresponding ones from α1 subunit makes α2 receptors sensitive to the potentiation by ginkgolic acid. Сurrents, mediated by α2 mutant receptors, increased by 89±14% after application of ginkgolic acid. Similarly to α1 receptors α2 mutant receptors have shown a decrease in EC50 for glycine under the action of ginkgolic acid. Thus, subunit selectivity of the ginkgolic acid is in strong connection with three amino acid residues that are different in α1 and α2 subunits of glycine receptor.

Keywords: glycine receptor; ginkgolic acid; ionic currents; patch-clamp; point mutations.

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