Jan Jakubik
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Explore the profile of Jan Jakubik including associated specialties, affiliations and a list of published articles.
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38
Citations
288
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Recent Articles
1.
Janouskova-Randakova A, Mezeiova E, Blahova J, Chetverikov N, Dolejsi E, Nelic D, et al.
Biomed Pharmacother
. 2025 Mar;
185:117977.
PMID: 40088774
Antagonists with a long residence time at the receptors are desired for the possibility of reducing daily doses and side effects. KH-5 (1-{2-[4-(hexyloxy)benzoyloxy]ethyl}-1-methyl-1,2,3,6-tetrahydropyridin-1-ium iodide) is the long-acting M-preferring bitopic muscarinic...
2.
Morales P, Scharf M, Bermudez M, Egyed A, Franco R, Hansen O, et al.
Br J Pharmacol
. 2024 Sep;
PMID: 39261899
Class A G protein-coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target...
3.
Nelic D, Chetverikov N, Hochmalova M, Diaz C, Dolezal V, Boulos J, et al.
Sci Rep
. 2024 Apr;
14(1):9652.
PMID: 38671143
Selective activation of individual subtypes of muscarinic receptors is a promising way to safely alleviate a wide range of pathological conditions in the central nervous system and the periphery as...
4.
Randakova A, Nelic D, Jakubik J
Sci Rep
. 2023 Oct;
13(1):17587.
PMID: 37845324
Agonist efficacy denoting the "strength" of agonist action is a cornerstone in the proper assessment of agonist selectivity and signalling bias. The simulation models are very accurate but complex and...
5.
Szczurowska E, Szanti-Pinter E, Chetverikov N, Randakova A, Kudova E, Jakubik J
Int J Mol Sci
. 2023 Jan;
24(1).
PMID: 36613951
Muscarinic acetylcholine receptors expressed in the central nervous system mediate various functions, including cognition, memory, or reward. Therefore, muscarinic receptors represent potential pharmacological targets for various diseases and conditions, such...
6.
Jakubik J, Randakova A
Expert Opin Drug Discov
. 2022 Nov;
17(11):1181-1191.
PMID: 36369915
Introduction: Accurate ranking of efficacies and potencies of agonists is essential in the discovery of new selective agonists. For the purpose of system-independent ranking of agonists, the operational model of...
7.
Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids
Szczurowska E, Szanti-Pinter E, Randakova A, Jakubik J, Kudova E
Int J Mol Sci
. 2022 Nov;
23(21).
PMID: 36361865
Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various internal diseases, as well as psychiatric and neurologic conditions. Cholesterol,...
8.
Randakova A, Nelic D, Hochmalova M, Zimcik P, Mulenga M, Boulos J, et al.
Int J Mol Sci
. 2021 Sep;
22(18).
PMID: 34576254
A complex evaluation of agonist bias at G-protein coupled receptors at the level of G-protein classes and isoforms including non-preferential ones is essential for advanced agonist screening and drug development....
9.
Dolejsi E, Szanti-Pinter E, Chetverikov N, Nelic D, Randakova A, Dolezal V, et al.
Neuropharmacology
. 2021 Sep;
199:108798.
PMID: 34555368
The membrane cholesterol was found to bind and modulate the function of several G-protein coupled receptors including muscarinic acetylcholine receptors. We investigated the binding of 20 steroidal compounds including neurosteroids...
10.
Dolejsi E, Chetverikov N, Szanti-Pinter E, Nelic D, Randakova A, Dolezal V, et al.
Biochem Pharmacol
. 2021 Jul;
192:114699.
PMID: 34324870
Endogenous neurosteroids and their synthetic analogues-neuroactive steroids-have been found to bind to muscarinic acetylcholine receptors and allosterically modulate acetylcholine binding and function. Using radioligand binding experiments we investigated their binding...