Connecting GSK-3β Inhibitory Activity with IKK-β or ROCK-1 Inhibition to Target Tau Aggregation and Neuroinflammation in Alzheimer’s Disease—Discovery, In Vitro and In Cellulo Activity of Thiazole-Based Inhibitors

Autor: Izabella Góral, Tomasz Wichur, Emilia Sługocka, Justyna Godyń, Natalia Szałaj, Paula Zaręba, Monika Głuch-Lutwin, Barbara Mordyl, Dawid Panek, Anna Więckowska

Publikováno v: Molecules, Vol 29, Iss 11, p 2616 (2024)

GSK-3β, IKK-β, and ROCK-1 kinases are implicated in the pathomechanism of Alzheimer’s disease due to their involvement in the misfolding and accumulation of amyloid β (Aβ) and tau proteins, as well as inflammatory processes. Among these kinases

Externí odkaz: https://doaj.org/article/d794b4a155cb4c9da646e809bc8a5781

Structure-guided design of N-methylpropargylamino-quinazoline derivatives as multipotent agents for the treatment of Alzheimer's disease

Autor: Barbora Svobodova, Lenka Pulkrabkova, Dawid Panek, Anna Misiachna, Marharyta Kolcheva, Rudolf Andrys, Jiri Handl, Jan Capek, Pavlina Nyvltova, Tomas Rousar, Lukas Prchal, Vendula Hepnarova, Martina Hrabinova, Lubica Muckova, Daniela Tosnerova, Galina Karabanovich, Vladimir Finger, Ondrej Soukup, Martin Horak, Jan Korabecny

Publikováno v: International Journal of Molecular Sciences; Volume 24; Issue 11; Pages: 9124

Alzheimer’s disease (AD) is a complex disease with an unknown etiology. Available treatments, limited to cholinesterase inhibitors and N-methyl-d-aspartate receptor (NMDAR) antagonists, provide symptomatic relief only. As single-target therapies ha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84cb799254ac08c27aef258d2c563f51
https://ruj.uj.edu.pl/xmlui/handle/item/312616

Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease

Autor: Anja Pišlar, Anna Więckowska, Barbara Malawska, Paula Zaręba, Raimon Sabaté, Dawid Panek, Jakub Jończyk, Tomasz Wichur, Natalia Szałaj, Anna Pasieka, Krzysztof Więckowski, Justyna Godyń, Marek Bajda

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1944-1952 (2020)

Effective therapy of Alzheimer’s disease (AD) requires treatment with a combination of drugs that modulate various pathomechanisms contributing to the disease. In our research, we have focused on the development of multi-target-directed ligands –

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::605fad8a83670327e0c22e4f705ac0bf
https://doi.org/10.1080/14756366.2020.1835882

Design, synthesis, and biological evaluation of 2-(benzylamino-2-hydroxyalkyl)isoindoline-1,3-diones derivatives as potential disease-modifying multifunctional anti-Alzheimer agents

Autor: Marek Bajda, Dawid Panek, Anna Pasieka, Justyna Godyń, Barbara Malawska, Damijan Knez, Jakub Jończyk, Anna Więckowska, Stanislav Gobec

Publikováno v: Molecules, vol. 23, no. 2, 347, 2018.
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
Molecules; Volume 23; Issue 2; Pages: 347
Molecules, Vol 23, Iss 2, p 347 (2018)

The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::adac0a0f1687fb51eab76153ea0d9ddd
https://repozitorij.uni-lj.si/Dokument.php?id=149289&dn=

New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition

Autor: Javier Egea, Daniel Diez-Iriepa, Barbara Mordyl, Alejandra Palomino-Antolín, Rim Malek, Lhassane Ismaili, Tereza Kobrlova, Justyna Godyń, Ondrej Soukup, José Marco-Contelles, Agata Siwek, Fakher Chabchoub, Ignacio Moraleda, Cristóbal de los Ríos, Dawid Panek, Céline Demougeot, Perle Totoson, Katarzyna Kieć-Kononowicz, Isabel Iriepa, Monika Głuch-Lutwin, Barbara Malawska, Raquel L Arribas

Publikováno v: Journal of Medicinal Chemistry. 62:11416-11422

New tritarget small molecules combining Ca2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound 3p has been identified as a very promising lead, showing good Ca2+ channels blockade activi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30367824b94baa33e4e87aec58b11b2e
https://doi.org/10.1021/acs.jmedchem.9b00937