Výsledky vyhledávání - "Milan Kožíšek"

Akademický článek

Structural and Thermodynamic Analysis of the Resistance Development to Pimodivir (VX-787), the Clinical Inhibitor of Cap Binding to PB2 Subunit of Influenza A Polymerase

Autor: Jiří Gregor, Kateřina Radilová, Jiří Brynda, Jindřich Fanfrlík, Jan Konvalinka, Milan Kožíšek

Publikováno v: Molecules, Vol 26, Iss 4, p 1007 (2021)

Influenza A virus (IAV) encodes a polymerase composed of three subunits: PA, with endonuclease activity, PB1 with polymerase activity and PB2 with host RNA five-prime cap binding site. Their cooperation and stepwise activation include a process calle

Externí odkaz: https://doaj.org/article/f2ea056deec24d22be14247821fb4095

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Ligand Strain and Its Conformational Complexity Is a Major Factor in the Binding of Cyclic Dinucleotides to STING Protein

Autor: Miroslav Smola, Ondrej Gutten, Milan Dejmek, Milan Kožíšek, Thomas Evangelidis, Zahra Aliakbar Tehrani, Barbora Novotná, Radim Nencka, Gabriel Birkuš, Lubomír Rulíšek, Evzen Boura

Publikováno v: Angewandte Chemie (International Ed. in English)

STING (stimulator of interferon genes) is a key regulator of innate immunity that has recently been recognized as a promising drug target. STING is activated by cyclic dinucleotides (CDNs) which eventually leads to expression of type I interferons an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eee445ddb3d2d83a85e47330275e3e4
https://doi.org/10.1002/anie.202016805

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Protein–Ligand Interactions in the STING Binding Site Probed by Rationally Designed Single-Point Mutations: Experiment and Theory

Autor: Miroslav Smola, Martin Zavřel, Gabriel Birkus, Vilém Charvát, Milan Kožíšek, Ondrej Gutten, Zahra Aliakbar Tehrani, Lubomír Rulíšek, Zdeněk Vavřina, Evzen Boura

Publikováno v: Biochemistry. 60:607-620

STING protein (stimulator of interferon genes) plays an important role in the innate immune system. A number of potent compounds regulating its activity have been reported, mostly derivatives of cyclic dinucleotides (CDNs), natural STING agonists. He

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8fcfa42287fa3c027f0680e8901d29b
https://doi.org/10.1021/acs.biochem.0c00949

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Akademický článek

Kinetic, Thermodynamic, and Structural Analysis of Drug Resistance Mutations in Neuraminidase from the 2009 Pandemic Influenza Virus

Autor: Jana Pokorná, Petr Pachl, Elena Karlukova, Jakub Hejdánek, Pavlína Řezáčová, Aleš Machara, Jason Hudlický, Jan Konvalinka, Milan Kožíšek

Publikováno v: Viruses, Vol 10, Iss 7, p 339 (2018)

Neuraminidase is the main target for current influenza drugs. Reduced susceptibility to oseltamivir, the most widely prescribed neuraminidase inhibitor, has been repeatedly reported. The resistance substitutions I223V and S247N, alone or in combinati

Externí odkaz: https://doaj.org/article/44eddd899f814570bf7ec6d9a06db19a

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Thermodynamic and structural characterization of an optimized peptide-based inhibitor of the influenza polymerase PA-PB1 subunit interaction

Autor: Kateřina Radilová, Václav Zima, Michal Kráľ, Aleš Machara, Pavel Majer, Jan Hodek, Jan Weber, Jiří Brynda, Timotej Strmeň, Jan Konvalinka, Milan Kožíšek

Publikováno v: Antiviral Research. 208:105449

Influenza virus causes severe respiratory infection in humans. Current antivirotics target three key proteins in the viral life cycle: neuraminidase, the M2 channel and the endonuclease domain of RNA-dependent-RNA polymerase. Due to the development o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7e90cf032c32ebb4014d2e5f1ce2334
https://doi.org/10.1016/j.antiviral.2022.105449

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Synthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors

Autor: Martin Dračínský, Aleš Machara, Milan Kožíšek, Pavel Majer, Robert Reiberger, Jiří Brynda, Václav Zima, Kateřina Radilová, Michal Kráľ, Jan Konvalinka

Publikováno v: International Journal of Molecular Sciences, Vol 22, Iss 7735, p 7735 (2021)
International Journal of Molecular Sciences
Volume 22
Issue 14

The part of the influenza polymerase PA subunit featuring endonuclease activity is a target for anti-influenza therapies, including the FDA-approved drug Xofluza. A general feature of endonuclease inhibitors is their ability to chelate Mg2+ or Mn2+ i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4e368bc3bf7ce70800472cee81f2cf7
https://www.mdpi.com/1422-0067/22/14/7735

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Structural and Thermodynamic Analysis of the Resistance Development to Pimodivir (VX-787), the Clinical Inhibitor of Cap Binding to PB2 Subunit of Influenza A Polymerase

Autor: Jindřich Fanfrlík, Jiří Brynda, Jan Konvalinka, Milan Kožíšek, Jiří Gregor, Kateřina Radilová

Publikováno v: Molecules, Vol 26, Iss 1007, p 1007 (2021)
Molecules
Volume 26
Issue 4

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80ba01b38e14fac17a37f44a5071fb80
https://www.mdpi.com/1420-3049/26/4/1007

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structural characterization of the interaction between the C-terminal domain of the influenza polymerase PA subunit and an optimized small peptide inhibitor

Autor: Jan Hodek, Jakub Hejdánek, Ales Machara, Jan Konvalinka, Milan Kožíšek, Jan Weber, Pavlína Řezáčová, Kateřina Radilová, Petr Pachl

Publikováno v: Antiviral research. 185

Influenza viruses can cause severe respiratory infections in humans, leading to nearly half a million deaths worldwide each year. Improved antiviral drugs are needed to address the threat of development of novel pandemic strains. Current therapeutic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76abffb793ac6b35b0880f59a029f9f3
https://pubmed.ncbi.nlm.nih.gov/33166574

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Rhomboid intramembrane protease YqgP licenses bacterial membrane protein quality control as adaptor of FtsH AAA protease

Autor: Rozálie Hexnerová, Mathieu Baudet, Thierry Doan, Jordan Delisle, Anne Galinier, Baptiste Cordier, Jakub Began, Vaclav Veverka, Kvido Strisovsky, Milan Kožíšek, Petra Rampírová, Yohann Couté, Jana Březinová, Pavel Srb

Publikováno v: EMBO Journal
EMBO Journal, 2020, ⟨10.15252/embj.2019102935⟩
EMBO Journal, EMBO Press, 2020, ⟨10.15252/embj.2019102935⟩
The EMBO Journal

Magnesium homeostasis is essential for life and depends on magnesium transporters, whose activity and ion selectivity need to be tightly controlled. Rhomboid intramembrane proteases pervade the prokaryotic kingdom, but their functions are largely elu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bf440d8169298428647796d6463e45e
https://hal.science/hal-02439524/file/Began_et_al-2020-The_EMBO_Journal.pdf

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Investigation of flexibility of neuraminidase 150-loop using tamiflu derivatives in influenza A viruses H1N1 and H5N1

Autor: Petr Pachl, Jana Pokorná, Ales Machara, Milan Kožíšek, Pavlína Řezáčová, Pavel Majer, Kateřina Rojíková, Václav Navrátil, Carlos Berenguer Albiñana, Jason Hudlicky, Jan Konvalinka, Václav Zima

Publikováno v: Bioorganicmedicinal chemistry. 27(13)

This study focuses on design, synthesis and in vitro evaluation of inhibitory potency of two series of sialylmimetic that target an exosite ("150-cavity") adjacent to the active site of influenza neuraminidases from A/California/07/2009 (H1N1) pandem

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfddee6b55c0413d3e34bdcbcaeb476c
https://pubmed.ncbi.nlm.nih.gov/31128993

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