Projects funded by the NCN


Information on the principal investigator and host institution

Information of the project and the call

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Selective inhibitors of γ-aminobutyric acid (GABA) transporter subtype 3 (GAT3) as a new pharmacological tools and a chance for a novel therapy of GABA-related disorders.

2021/41/B/NZ7/02825

Keywords:

medicinal chemistry drug discovery γ-butyric acid γ-aminobutyric acid transporters inhibitors of γ-aminobutyric acid transporters, selective inhibitors of the GAT3-type transporter epilepsy neuropathic pain Alzheimer's disease

Descriptors:

  • NZ7_014:
  • NZ3_007:
  • ST4_008:

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Uniwersytet Jagielloński, Collegium Medicum

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr Dawid Marcin Panek 

Number of co-investigators in the project: 11

Call: OPUS 21 - announced on 2021-03-15

Amount awarded: 1 684 200 PLN

Project start date (Y-m-d): 2022-02-07

Project end date (Y-m-d): 2026-02-06

Project duration:: 48 months (the same as in the proposal)

Project status: Project completed

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Information in the final report

  • Publication in academic press/journals (3)
  1. Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease
    Authors:
    Paula Zaręba, Kamil Łątka, Gabriela Mazur, Beata Gryzło, Anna Pasieka, Justyna Godyń, Dawid Panek, Anna Skrzypczak-Wiercioch, Georg C Höfner, Gniewomir Latacz, Maciej Maj, Alba Espargaró, Raimon Sabaté, Krzysztof Jóźwiak, Klaus T Wanner, Kinga Sałat, Barbara Malawska, Katarzyna Kulig, Marek Bajda
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2023, tom: 261, strony: 115832), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2023.115832 - link to the publication
  2. Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies
    Authors:
    Dawid Panek, Anna Pasieka, Gniewomir Latacz, Paula Zaręba, Michał Szczęch, Justyna Godyń, Fabien Chantegreil, Florian Nachon, Xavier Brazzolotto, Anna Skrzypczak-Wiercioch, Maria Walczak, Magdalena Smolik, Kinga Sałat, Georg Höfner, Klaus Wanner, Anna Więckowska, Barbara Malawska
    Academic press:
    The European Journal of Medicinal Chemistry (rok: 2023, tom: 249, strony: 115135), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2023.115135 - link to the publication
  3. Multifunctional, Fluorene-Based Modulator of Cholinergic and GABAergic Neurotransmission as a Novel Drug Candidate for Palliative Treatment of Alzheimer's Disease
    Authors:
    Dawid Panek, Anna Pasieka, Jakub Jończyk, Milena Gawlińska, Paula Zaręba, Agata Siwek, Małgorzata Wolak, Barbara Mordyl, Monika Głuch-Lutwin, Gniewomir Latacz, Xavier Brazzolotto, Fabien Chantegreil, Florian Nachon, Jana Zdarova Karasova, Jaroslav Pejchal, Martin Mzik, Vit Sestak, Lukas Prchal, Jitka Odvarkova, Ondrej Soukup, Jan Korabecny, Ales Sorf, Marie Hamsikova, Lucie Zemanova, Lubica Muckova, Nela Vánova, Pola Dryja, Kinga Sałat, Georg Höfner, Klaus Wanner, Anna Więckowska, Barbara Malawska
    Academic press:
    Angewandte Chemie International Edition (rok: 2024, tom: 64, strony: e202420510), Wydawca: Willey
    Status:
    Published
    DOI:
    10.1002/anie.202420510 - link to the publication