Počet záznamů: 1
Distributions of therapeutically promising neurosteroids in cellular membranes
- 1.
SYSNO ASEP 0475164 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Distributions of therapeutically promising neurosteroids in cellular membranes Tvůrce(i) Riedlová, Kamila (UOCHB-X)
Nekardová, Michaela (UOCHB-X) RID
Kačer, P. (CZ)
Syslová, K. (CZ)
Vazdar, M. (HR)
Jungwirth, Pavel (UOCHB-X) RID, ORCID
Kudová, Eva (UOCHB-X) RID, ORCID
Cwiklik, Lukasz (UFCH-W) RID, ORCIDZdroj.dok. Chemistry and Physics of Lipids. - : Elsevier - ISSN 0009-3084
Roč. 203, Mar (2017), s. 78-86Poč.str. 9 s. Jazyk dok. eng - angličtina Země vyd. IE - Irsko Klíč. slova steroids ; N-methyl-D-aspartate receptors ; membranes ; molecular dynamics ; chromatography Vědní obor RIV CF - Fyzikální chemie a teoretická chemie Obor OECD Physical chemistry Vědní obor RIV – spolupráce Ústav fyzikální chemie J.Heyrovského - Fyzikální chemie a teoretická chemie CEP TE01020028 GA TA ČR - Technologická agentura ČR GAP303/12/1464 GA ČR - Grantová agentura ČR GA15-14292S GA ČR - Grantová agentura ČR GBP208/12/G016 GA ČR - Grantová agentura ČR Institucionální podpora UOCHB-X - RVO:61388963 ; UFCH-W - RVO:61388955 UT WOS 000395725500009 EID SCOPUS 85010992297 DOI 10.1016/j.chemphyslip.2016.12.004 Anotace Interactions of two neurosteroids, inhibiting membrane-bound N-Methyl-D-aspartate receptors, with phospholipid membranes are studied. Namely, endogenous pregnanolone sulfate is compared with pregnanolone glutamate, the latter being a novel synthetic steroidal inhibitor of these receptors with potential pharmaceutical use. Molecular-level details of steroid-phospholipid membranes interactions are scrutinized employing molecular dynamics simulations supported by quantum chemical calculations to assess steroid lipophilicity. Moreover, permeability of both species across membranes is experimentally evaluated by immobilized artificial membrane chromatography. We demonstrate that while there is no significant difference of lipophilicity and membrane permeability between the two steroids, they differ significantly regarding detailed localization in phospholipid membranes. The bulky glutamate moiety of pregnanolone glutamate is flexible and well exposed to the water phase while the sulfate group of pregnanolone sulfate is hidden in the membrane headgroup region. This dissimilarity of behavior in membranes can potentially account for the observed different activities of the two steroids toward membrane-bound N-Methyl-D-aspartate receptors. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2018
Počet záznamů: 1