Počet záznamů: 1  

Computational investigation on the effect of the peptidomimetic inhibitors (NPT100-18A and NPT200-11) on the α-synuclein and lipid membrane interactions

  1. 1.
    SYSNO ASEP0578423
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevComputational investigation on the effect of the peptidomimetic inhibitors (NPT100-18A and NPT200-11) on the α-synuclein and lipid membrane interactions
    Tvůrce(i) Das, D. (IN)
    Bharadwaz, Priyam (UFCH-W) SAI
    Mattaparthi, V. S. K. (IN)
    Zdroj.dok.Journal of Biomolecular Structure & Dynamics. - : Taylor & Francis - ISSN 0739-1102
    (2023)
    Poč.str.10 s.
    Jazyk dok.eng - angličtina
    Země vyd.GB - Velká Británie
    Klíč. slovamolecular-dynamics simulations ; lewy body disease ; parkinsons-disease ; force-field ; basis-sets ; system ; oligomerization ; accumulation ; mutations ; mechanism ; alpha-Synuclein aggregation ; membrane dynamics ; dft ; npt100-18a ; npt200-11
    Obor OECDPhysical chemistry
    Způsob publikováníOmezený přístup
    Institucionální podporaUFCH-W - RVO:61388955
    UT WOS001077480000001
    EID SCOPUS85173948923
    DOI10.1080/07391102.2023.2262599
    AnotaceParkinson's disease (PD) is associated with alpha-synuclein (alpha-Syn), a presynaptic protein that binds to cell membranes. The molecular pathophysiology of PD most likely begins with the binding of alpha-Syn to membranes. Recently, two peptidomimetic inhibitors (NPT100-18A and NPT200-11) were identified to potentially interact with alpha-Syn and affect the interaction of alpha-Syn with the membrane. In this study, the effect of the two peptidomimetic inhibitors on the alpha-Syn-membrane interaction was demonstrated. DFT calculations were performed for optimization of the two inhibitors, and the nucleophilicity (N) and electrophilicity (omega) of NPT100-18A and NPT200-11 were calculated to be 3.90 and 3.86 (N), 1.06 and 1.04 (omega), respectively. Using the docking tool (CB-dock2), the two alpha-Syn-peptidomimetic inhibitor complexes (alpha-Syn-NPT100-18A and alpha-Syn-NPT200-11) have been prepared. Then all-atom molecular dynamics (MD) simulation was carried out on the alpha-Syn (control), alpha-Syn-NPT100-18A and alpha-Syn-NPT200-11 complex systems in presence of DOPE: DOPS: DOPC (5:3:2) lipid bilayer. From the conformational dynamics analysis, the 3-D structure of alpha-Syn was found to be stable, and the helices present in the regions (1-37) and (45-95) of alpha-Syn were found to be retained in the presence of the two peptidomimetic inhibitors. The electron density profile analysis revealed the binding modes of NAC and C-terminal region of alpha-Syn (in the presence of NPT200-11 inhibitor) with lipid membrane are in the close vicinity from the lipid bilayer centre. Our findings in this study on alpha-Syn-membrane interactions may be useful for developing a new therapeutic approach for treating PD and other neurodegenerative disorders.
    PracovištěÚstav fyzikální chemie J.Heyrovského
    KontaktMichaela Knapová, michaela.knapova@jh-inst.cas.cz, Tel.: 266 053 196
    Rok sběru2025
    Elektronická adresahttps://www.tandfonline.com/doi/abs/10.1080/07391102.2023.2262599
Počet záznamů: 1  

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