Personal information

molecular pharmacology, neurochemistry, neurosciences, physiology
Czech Republic

Activities

Employment (1)

Institute of Physiology CAS: Praha, CZ

2001-05-01 to present | researcher/scientist (Neurochemistry)
Employment
Source: Self-asserted source
Jan Jakubik

Education and qualifications (2)

First Faculty of Medicine, Charles University: Praha, CZ

1993-10-01 to 1997-06-30 | PhD
Education
Source: Self-asserted source
Jan Jakubik

Faculty of Science, Charles University: Praha, CZ

1988-10-01 to 1993-06-30 | MSc.
Education
Source: Self-asserted source
Jan Jakubik

Funding (4)

Structure-activity guided design of novel long-acting antagonists of muscarinic receptors

2023-01 to 2025-12 | Grant
Grantová Agentura České Republiky (Praha, CZ)
GRANT_NUMBER:

23-04670S

Source: Self-asserted source
Jan Jakubik

Národní ústav pro neurologický výzkum

2022-07 to 2025-12 | Grant
Ministerstvo Školství, Mládeže a Tělovýchovy (Praha, CZ)
Part of GRANT_NUMBER:

LX22NPO5107

Source: Self-asserted source
Jan Jakubik

Molecular basis of functional selectivity of N-substituted tetrahydropyridinium salts at muscarinic receptors

2019-01 to 2021-12 | Grant
Grantová Agentura České Republiky (Praha, CZ)
GRANT_NUMBER:

19-05318S

Source: Self-asserted source
Jan Jakubik

Molecular basis of functional selectivity of N-substituted tetrahydropyridinium salts at muscarinic receptors

2017-01 to 2019-12 | Grant
Grantová Agentura České Republiky (Praha, CZ)
GRANT_NUMBER:

17-16182S

Source: Self-asserted source
Jan Jakubik

Works (50 of 70)

Items per page:
Page 1 of 2

A critical re-evaluation of the slope factor of the operational model of agonism: When to exponentiate operational efficacy

Scientific Reports
2023-10-16 | Journal article
Part of ISSN: 2045-2322
Contributors: Alena Randáková; Dominik Nelic; Jan Jakubík
Source: Self-asserted source
Jan Jakubik

Modulation of Muscarinic Signalling in the Central Nervous System by Steroid Hormones and Neurosteroids

International Journal of Molecular Sciences
2022-12-28 | Journal article
Contributors: Ewa Szczurowska; Eszter Szánti-Pintér; Nikolai Chetverikov; Alena Randáková; Eva Kudová; Jan Jakubík
Source: check_circle
Crossref

Insights into the operational model of agonism of receptor dimers

Expert Opinion on Drug Discovery
2022-11-02 | Journal article
Contributors: Jan Jakubík; Alena Randáková
Source: check_circle
Crossref

Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids

International Journal of Molecular Sciences
2022-10-28 | Journal article
Contributors: Ewa Szczurowska; Eszter Szánti-Pintér; Alena Randáková; Jan Jakubík; Eva Kudova
Source: check_circle
Crossref
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Neurosteroids and steroid hormones are allosteric modulators of muscarinic receptors

Neuropharmacology
2021-11 | Journal article
Contributors: Eva Dolejší; Eszter Szánti-Pintér; Nikolai Chetverikov; Dominik Nelic; Alena Randáková; Vladimír Doležal; Eva Kudová; Jan Jakubík
Source: check_circle
Crossref

Fusion with Promiscuous Gα16 Subunit Reveals Signaling Bias at Muscarinic Receptors

International Journal of Molecular Sciences
2021-09-18 | Journal article
Contributors: Alena Randáková; Dominik Nelic; Martina Hochmalová; Pavel Zimčík; Mutale Jane Mulenga; John Boulos; Jan Jakubík
Source: check_circle
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Guanidine Derivatives: How Simple Structural Modification of Histamine H3R Antagonists Has Led to the Discovery of Potent Muscarinic M2R/M4R Antagonists

ACS Chemical Neuroscience
2021-07-07 | Journal article
Contributors: Marek Staszewski; Dominik Nelic; Jakub Jończyk; Mariam Dubiel; Annika Frank; Holger Stark; Marek Bajda; Jan Jakubik; Krzysztof Walczyński
Source: check_circle
Crossref

Critical re-evaluation of the slope factor of the operational model of agonism: Do not exponentiate operational efficacy

2021-04-09 | Preprint
Contributors: Jan Jakubík
Source: check_circle
Crossref

Allosteric Modulation of GPCRs of Class A by Cholesterol

International Journal of Molecular Sciences
2021-02-16 | Journal article
Contributors: Jan Jakubík; Esam E. El-Fakahany
Source: check_circle
Crossref
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Steroids as the novel class of high-affinity allosteric modulators of muscarinic receptors

2021-02-04 | Preprint
Contributors: Eva Dolejší; Eszter Szánti-Pintér; Nikolai Chetverikov; Dominik Nelic; Alena Randáková; Vladimír Doležal; Eva Kudová; Jan Jakubik
Source: check_circle
Crossref

Allosteric Modulation of GPCRs of Class A by Cholesterol

2021-01-21 | Other
Contributors: Jan Jakubík; Esam E. El-Fakahany
Source: check_circle
Crossref
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The operational model of allosteric modulation of pharmacological agonism

Scientific Reports
2020-12 | Journal article
Source: Self-asserted source
Jan Jakubik

Novel M2‐selective, Gi‐biased agonists of muscarinic acetylcholine receptors

British Journal of Pharmacology
2020-05 | Journal article
Contributors: Alena Randáková; Dominik Nelic; Dana Ungerová; Peter Nwokoye; Qiwen Su; Vladimír Doležal; Esam E. El‐Fakahany; John Boulos; Jan Jakubík
Source: check_circle
Crossref

Agonist-Specific Conformations of the M2 Muscarinic Acetylcholine Receptor Assessed by Molecular Dynamics

Journal of Chemical Information and Modeling
2020-04-27 | Journal article
Contributors: Alena Randáková; Dominik Nelic; Vladimír Doležal; Esam E. El-Fakahany; John Boulos; Jan Jakubík
Source: check_circle
Crossref

Current Advances in Allosteric Modulation of Muscarinic Receptors

Biomolecules
2020-02-18 | Journal article
Source: Self-asserted source
Jan Jakubik

Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators

PLOS ONE
2019-03-27 | Journal article
Contributors: Jan Jakubík; Elena Papaleo; Alena Randáková; Esam E. El-Fakahany; Vladimír Doležal
Source: check_circle
Crossref
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Applications and limitations of fitting of the operational model to determine relative efficacies of agonists

Scientific Reports
2019-03-15 | Journal article
Contributors: Jan Jakubík; Alena Randáková; Vladimír Rudajev; Pavel Zimčík; Esam E. El-Fakahany; Vladimír Doležal
Source: check_circle
Crossref
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Role of membrane cholesterol in differential sensitivity of muscarinic receptor subtypes to persistently bound xanomeline

Neuropharmacology
2018 | Journal article
EID:

2-s2.0-85041673319

Contributors: Randáková, A.; Dolejší, E.; Rudajev, V.; Zimčík, P.; Doležal, V.; El-Fakahany, E.E.; Jakubík, J.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Novel long‐acting antagonists of muscarinic ACh receptors

British Journal of Pharmacology
2018-05 | Journal article
Contributors: Alena Randáková; Vladimír Rudajev; Vladimír Doležal; John Boulos; Jan Jakubík
Source: check_circle
Crossref
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Binding of N-methylscopolamine to the allosteric site of M2 muscarinic acetylcholine receptor

Journal of Neurochemistry
2017 | Journal article
WOSUID:

WOS:000407426000083

Contributors: Jakubik, Jan; Randakova, Alena; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID

Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors

Scientific Reports
2017 | Journal article
WOSUID:

WOS:000391918500001

Contributors: Jakubik, Jan; Randakova, Alena; Zimcik, Pavel; El-Fakahany, Esam E.; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Receptor - membrane interactions as a potential basis of functional selectivity of xanomeline for M1 and M4 muscarinic receptors

Journal of Neurochemistry
2017 | Journal article
WOSUID:

WOS:000407426000051

Contributors: Randakova, Alena; Zimcik, Pavel; Dolejsi, Eva; Dolezal, Vladimir; Jakubik, Jan
Source: Self-asserted source
Jan Jakubik via ResearcherID

Synthesis of novel and functionally selective non-competitive muscarinic antagonists as chemical probes.

Chemical biology & drug design
2017 | Journal article
WOSUID:

MEDLINE:28646631

Contributors: Boulos, John F; Jakubik, Jan; Boulos, John M; Randakova, Alena; Momirov, Jelena
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Allosteric Modulation of Muscarinic Receptors

Muscarinic Receptor: From Structure To Animal Models
2016 | Book chapter
WOSUID:

WOS:000366481100008

Contributors: Jakubik, Jan; El-Fakahany, Esam E.; Myslivecek, J; Jakubik, J
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Muscarinic Receptor: From Structure to Animal Models

Muscarinic Receptor: From Structure To Animal Models
2016 | Book chapter
WOSUID:

WOS:000366481100018

Contributors: Myslivecek, J; Jakubik, J
Source: Self-asserted source
Jan Jakubik via ResearcherID

Radioligand Binding at Muscarinic Receptors

Muscarinic Receptor: From Structure To Animal Models
2016 | Book chapter
WOSUID:

WOS:000366481100005

Contributors: El-Fakahany, Esam E.; Jakubik, Jan; Myslivecek, J; Jakubik, J
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Classical and atypical agonists activate M1 muscarinic acetylcholine receptors through common mechanisms

Journal of Neurochemistry
2015 | Journal article
WOSUID:

WOS:000360206300349

Contributors: Jakubik, J.; Randakova, A.; Zimcik, P.; El-Fakahany, E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID

Lipid-Based Diets Improve Muscarinic Neurotransmission in the Hippocampus of Transgenic APPswe/PS1dE9 Mice

Current Alzheimer Research
2015 | Journal article
WOSUID:

WOS:000366135300002

Contributors: Janickova, Helena; Rudajev, Vladimir; Dolejsi, Eva; Koivisto, Hennariikka; Jakubik, Jan; Tanila, Heikki; El-Fakahany, Esam E.; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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M1 muscarinic receptors newly incorporated into plasma membrane of CHO cells demonstrate alterations in agonist binding properties

Journal of Neurochemistry
2015 | Journal article
WOSUID:

WOS:000360206300398

Contributors: Dolejsi, E.; Janickova, H.; Jakubik, J.; Esam, E. El-Fakahany; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID

Towards predictive docking at aminergic G-protein coupled receptors

Journal of Molecular Modeling
2015 | Journal article
WOSUID:

WOS:000364527300004

Contributors: Jakubik, Jan; El-Fakahany, Esam E.; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Classical and atypical agonists activate M1 muscarinic acetylcholine receptors through common mechanisms

Pharmacological Research
2015-07 | Journal article
Contributors: Alena Randáková; Eva Dolejší; Vladimír Rudajev; Pavel Zimčík; Vladimír Doležal; Esam E. El-Fakahany; Jan Jakubík
Source: check_circle
Crossref
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Long-Term Activation upon Brief Exposure to Xanomleline Is Unique to M-1 and M-4 Subtypes of Muscarinic Acetylcholine Receptors

Plos One
2014 | Journal article
DOI:

10.1371/journal.pone.0088910

Contributors: Santruckova, Eva; Dolezal, Vladimir; El-Fakahany, Esam E.; Jakubik, Jan
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Molecular mechanisms of methoctramine binding and selectivity at muscarinic acetylcholine receptors

Molecular Pharmacology
2014 | Journal article
EID:

2-s2.0-84903585210

Contributors: Jakubík, J.; Zimčík, P.; Randáková, A.; Fuksová, K.; El-Fakahany, E.E.; Doležal, V.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Outline of therapeutic interventions with muscarinic receptor-mediated transmission

Physiological Research
2014 | Journal article
EID:

2-s2.0-84897640586

Contributors: Jakubík, J.; Šantrůcková, E.; Randáková, A.; Janíčková, H.; Zimčík, P.; Rudajev, V.; Michal, P.; El-Fakahany, E.E.; Doležal, V.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Mechanisms of activation of the M1 muscarinic receptor by atypical and classical agonists

Journal of Neurochemistry
2013 | Journal article
WOSUID:

WOS:000316961700320

Contributors: Randakova, A.; Santruckova, E.; Zimcik, P.; Jakubik, J.; El-Fakahany, E. E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID

On homology modeling of the M-2 muscarinic acetylcholine receptor subtype

Journal of Computer-Aided Molecular Design
2013 | Journal article
DOI:

10.1007/s10822-013-9660-8

Contributors: Jakubik, Jan; Randakova, Alena; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Prolonged A beta 1-42 treatment does not influence membrane localization of M1 muscarinic receptors expressed in CHO cells

Journal of Neurochemistry
2013 | Journal article
Contributors: Janickova, H.; Rudajev, V.; Jakubik, J.; El-Fakahany, E. E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID

Subtype differences in effects of brief exposure to xanomeline on binding and activation of muscarinic acetylcholine

Journal of Neurochemistry
2013 | Journal article
Contributors: Santruckova, E.; Jakubik, J.; El-Fakahany, E. E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID

Synthesis of N-Substituted Piperidine Salts as Potential Muscarinic Ligands for Alzheimer's Applications

Journal of Heterocyclic Chemistry
2013 | Journal article
DOI:

10.1002/jhet.1742

Contributors: Boulos, John; Jakubik, Jan; Randakova, Alena; Avila, Cristina
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Uncoupling of M1 muscarinic receptor/G-protein interaction by amyloid beta(1-42)

Neuropharmacology
2013 | Journal article
DOI:

10.1016/j.neuropharm.2012.11.014

Contributors: Janickova, Helena; Rudajev, Vladimir; Zimcik, Pavel; Jakubik, Jan; Tanila, Heikki; El-Fakahany, Esam E.; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Progressive decline of muscarinic neurotransmissin in cerebral cortex of transgenic APPswe/PS1dE9 mouse model of Alzheimer's disease

Journal of Molecular Neuroscience
2012 | Journal article
Contributors: Machova, E.; Janickova, H.; Rudajev, V; Michal, P.; Jakubik, J.; Oksman, M.; Koivisto, H.; Iivonen, H.; Tanila, H.; Dolczal, V
Source: Self-asserted source
Jan Jakubik via ResearcherID

Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy

British Journal of Pharmacology
2011 | Journal article
DOI:

10.1111/j.1476-5381.2010.01081.x

Contributors: Jakubik, J.; Janickova, H.; El-Fakahany, E. E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Subtype Differences in Pre-Coupling of Muscarinic Acetylcholine Receptors

Plos One
2011 | Journal article
DOI:

10.1371/journal.pone.0027732

Contributors: Jakubik, Jan; Janickova, Helena; Randakova, Alena; El-Fakahany, Esam E.; Dolezal, Vladimir
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Allosteric modulation of muscarinic acetylcholine receptors

Pharmaceuticals
2010 | Journal article
EID:

2-s2.0-77957282651

Contributors: Jakubík, J.; El-Fakahany, E.E.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Pharmacological Evaluation of the Long-Term Effects of Xanomeline on the M(1) Muscarinic Acetylcholine Receptor

Plos One
2010 | Journal article
DOI:

10.1371/journal.pone.0015722

Contributors: Grant, Marianne K. O.; Noetzel, Meredith J.; De Lorme, Kayla C.; Jakubik, Jan; Dolezal, Vladimir; El-Fakahany, Esam E.
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors

BMC Pharmacology
2009 | Journal article
EID:

2-s2.0-74549198652

Contributors: Jakubík, J.; Randáková, A.; El-Fakahany, E.E.; Doležal, V.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Weak toxin WTX from Naja kaouthia cobra venom interacts with both nicotinic and muscarinic acetylcholine receptors

Febs Journal
2009 | Journal article
DOI:

10.1111/j.1742-4658.2009.07203.x

Contributors: Mordvintsev, D. Y.; Polyak, Y. L.; Rodionov, D. I.; Jakubik, J.; Dolezal, V.; Karlsson, E.; Tsetlin, V. I.; Utkin, Y. N.
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Impairment of muscarinic transmission in transgenic APPswe/PS1dE9 mice

Neurobiology of Aging
2008 | Journal article
DOI:

10.1016/j.neurobiolaging.2006.10.029

Contributors: Machova, E.; Jakubik, J.; Michal, R.; Oksman, M.; Iivonen, H.; Tanila, H.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID
grade
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Importance and prospects for design of selective muscarinic agonists.

Physiological research / Academia Scientiarum Bohemoslovaca
2008 | Journal article
EID:

2-s2.0-62149119608

Contributors: Jakubík, J.; Michal, P.; Machová, E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via Scopus - Elsevier

Wash-resistantly bound xanomeline inhibits acetylcholine release by persistent activation of presynaptic M-2 and M-4 muscarinic receptors in rat brain

Journal of Pharmacology and Experimental Therapeutics
2007 | Journal article
DOI:

10.1124/jpet.107.122093

Contributors: Machova, E.; Jakubik, J.; El-Fakahany, E. E.; Dolezal, V.
Source: Self-asserted source
Jan Jakubik via ResearcherID
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Items per page:
Page 1 of 2

Peer review (5 reviews for 4 publications/grants)

Review activity for Heliyon. (1)
Review activity for Molecules. (2)
Review activity for Nature communications (1)
Review activity for Pharmacological Reports. (1)