-
Je něco špatně v tomto záznamu ?
Neurosteroids as positive and negative allosteric modulators of ligand-gated ion channels: P2X receptor perspective
S. Sivcev, E. Kudova, H. Zemkova
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články, přehledy, práce podpořená grantem
Odkazy
PubMed
37040816
DOI
10.1016/j.neuropharm.2023.109542
Knihovny.cz E-zdroje
- MeSH
- adenosintrifosfát metabolismus MeSH
- iontové kanály řízené ligandy * metabolismus MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- mozek metabolismus MeSH
- neurosteroidy * MeSH
- purinergní receptory P2X metabolismus MeSH
- purinergní receptory P2X2 metabolismus MeSH
- vazebná místa MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
Neurosteroids are steroids synthesized de novo in the brain from cholesterol in an independent manner from peripheral steroid sources. The term "neuroactive steroid" includes all steroids independent of their origin, and newly synthesized analogs of neurosteroids that modify neuronal activities. In vivo application of neuroactive steroids induces potent anxiolytic, antidepressant, anticonvulsant, sedative, analgesic and amnesic effects, mainly through interaction with the γ-aminobutyric acid type-A receptor (GABAAR). However, neuroactive steroids also act as positive or negative allosteric regulators on several ligand-gated channels including N-methyl-d-aspartate receptors (NMDARs), nicotinic acetylcholine receptors (nAChRs) and ATP-gated purinergic P2X receptors. Seven different P2X subunits (P2X1-7) can assemble to form homotrimeric or heterotrimeric ion channels permeable for monovalent cations and calcium. Among them, P2X2, P2X4, and P2X7 are the most abundant within the brain and can be regulated by neurosteroids. Transmembrane domains are necessary for neurosteroid binding, however, no generic motif of amino acids can accurately predict the neurosteroid binding site for any of the ligand-gated ion channels including P2X. Here, we will review what is currently known about the modulation of rat and human P2X by neuroactive steroids and the possible structural determinants underlying neurosteroid-induced potentiation and inhibition of the P2X2 and P2X4 receptors. This article is part of the Special Issue on "Purinergic Signaling: 50 years".
Faculty of Science Charles University Prague Czech Republic
Institute of Organic Chemistry and Biochemistry Czech Academy of Sciences Prague Czech Republic
Institute of Physiology Czech Academy of Sciences Prague Czech Republic
- 000
- 00000naa a2200000 a 4500
- 001
- bmc23010811
- 003
- CZ-PrNML
- 005
- 20230801132632.0
- 007
- ta
- 008
- 230718s2023 enk f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.1016/j.neuropharm.2023.109542 $2 doi
- 035 __
- $a (PubMed)37040816
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a enk
- 100 1_
- $a Sivcev, Sonja $u Institute of Physiology, Czech Academy of Sciences, Prague, Czech Republic; Faculty of Science, Charles University, Prague, Czech Republic
- 245 10
- $a Neurosteroids as positive and negative allosteric modulators of ligand-gated ion channels: P2X receptor perspective / $c S. Sivcev, E. Kudova, H. Zemkova
- 520 9_
- $a Neurosteroids are steroids synthesized de novo in the brain from cholesterol in an independent manner from peripheral steroid sources. The term "neuroactive steroid" includes all steroids independent of their origin, and newly synthesized analogs of neurosteroids that modify neuronal activities. In vivo application of neuroactive steroids induces potent anxiolytic, antidepressant, anticonvulsant, sedative, analgesic and amnesic effects, mainly through interaction with the γ-aminobutyric acid type-A receptor (GABAAR). However, neuroactive steroids also act as positive or negative allosteric regulators on several ligand-gated channels including N-methyl-d-aspartate receptors (NMDARs), nicotinic acetylcholine receptors (nAChRs) and ATP-gated purinergic P2X receptors. Seven different P2X subunits (P2X1-7) can assemble to form homotrimeric or heterotrimeric ion channels permeable for monovalent cations and calcium. Among them, P2X2, P2X4, and P2X7 are the most abundant within the brain and can be regulated by neurosteroids. Transmembrane domains are necessary for neurosteroid binding, however, no generic motif of amino acids can accurately predict the neurosteroid binding site for any of the ligand-gated ion channels including P2X. Here, we will review what is currently known about the modulation of rat and human P2X by neuroactive steroids and the possible structural determinants underlying neurosteroid-induced potentiation and inhibition of the P2X2 and P2X4 receptors. This article is part of the Special Issue on "Purinergic Signaling: 50 years".
- 650 _2
- $a krysa rodu Rattus $7 D051381
- 650 _2
- $a lidé $7 D006801
- 650 _2
- $a zvířata $7 D000818
- 650 12
- $a iontové kanály řízené ligandy $x metabolismus $7 D058446
- 650 12
- $a neurosteroidy $7 D000081227
- 650 _2
- $a purinergní receptory P2X $x metabolismus $7 D058469
- 650 _2
- $a mozek $x metabolismus $7 D001921
- 650 _2
- $a vazebná místa $7 D001665
- 650 _2
- $a adenosintrifosfát $x metabolismus $7 D000255
- 650 _2
- $a purinergní receptory P2X2 $x metabolismus $7 D058476
- 655 _2
- $a časopisecké články $7 D016428
- 655 _2
- $a přehledy $7 D016454
- 655 _2
- $a práce podpořená grantem $7 D013485
- 700 1_
- $a Kudova, Eva $u Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Prague, Czech Republic
- 700 1_
- $a Zemkova, Hana $u Institute of Physiology, Czech Academy of Sciences, Prague, Czech Republic. Electronic address: zemkova@biomed.cas.cz
- 773 0_
- $w MED00003497 $t Neuropharmacology $x 1873-7064 $g Roč. 234, č. - (2023), s. 109542
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/37040816 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y p $z 0
- 990 __
- $a 20230718 $b ABA008
- 991 __
- $a 20230801132629 $b ABA008
- 999 __
- $a ok $b bmc $g 1963310 $s 1197076
- BAS __
- $a 3
- BAS __
- $a PreBMC-MEDLINE
- BMC __
- $a 2023 $b 234 $c - $d 109542 $e 20230409 $i 1873-7064 $m Neuropharmacology $n Neuropharmacology $x MED00003497
- LZP __
- $a Pubmed-20230718