Výsledky vyhledávání - "Milan Kozisek"

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

Autor: E. Karlukova, Pavlina Rezacova, Petr Pachl, Jan Konvalinka, Jana Pokorná, Aleš Machara, J. Hudlicky, J. Hejdanek, Milan Kozisek

Publikováno v: Viruses
Volume 10
Issue 7
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://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdb02d6c5e32cbac256c06421664feb7
https://doi.org/10.3390/v10070339

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Design of HIV Protease Inhibitors Based on Inorganic Polyhedral Metallacarboranes

Autor: Jan Konvalinka, Jana Pokorná, Bohumír Grüner, Jaromír Plešek, Pavlina Rezacova, Heike Oberwinkler, Klára Grantz Šašková, Václav Šícha, Petr Cigler, Vladimír Král, Pavel Hobza, Hans-Georg Kräusslich, Martin Lepšík, Jindrich Fanfrlík, Juraj Sedlacek, Irena Sieglová, Milan Kozisek, Jan Rezac, Jiri Brynda

Publikováno v: Journal of Medicinal Chemistry. 52:7132-7141

HIV protease (HIV PR) is a primary target for anti-HIV drug design. We have previously identified and characterized substituted metallacarboranes as a new class of HIV protease inhibitors. In a structure-guided drug design effort, we connected the tw

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7caec979b1cc75b93e5985060eb0285
https://doi.org/10.1021/jm9011388

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Molecular Characterization of Clinical Isolates of Human Immunodeficiency Virus Resistant to the Protease Inhibitor Darunavir

Autor: Pavlina Rezacova, Jan Konvalinka, Ron M. Kagan, Tatyana Yashina, Jiri Brynda, Milan Kozisek, Klára Grantz Šašková

Publikováno v: Journal of Virology. 83:8810-8818

Darunavir is the most recently approved human immunodeficiency virus (HIV) protease (PR) inhibitor (PI) and is active against many HIV type 1 PR variants resistant to earlier-generation PIs. Darunavir shows a high genetic barrier to resistance develo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8239b6273177ca292375b28fe98fec0e
https://doi.org/10.1128/jvi.00451-09

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Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir

Autor: Jan Konvalinka, Jiri Brynda, Martin Lepšík, Pavlina Rezacova, Milan Kozisek, Ladislav Machala, Jana Václavíková, Ron M. Kagan, Klára Grantz Šašková

Publikováno v: Protein Science. 17:1555-1564

Lopinavir (LPV) is a second-generation HIV protease inhibitor (PI) designed to overcome resistance development in patients undergoing long-term antiviral therapy. The mutation of isoleucine at position 47 of the HIV protease (PR) to alanine is associ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2ad214b7e4d47bad36b0f3bc5dc37d2
https://doi.org/10.1110/ps.036079.108

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Crystal structures of the effector-binding domain of repressor Central glycolytic gene Regulator fromBacillus subtilisreveal ligand-induced structural changes upon binding of several glycolytic intermediates

Autor: Irena Sieglová, Milan Kozisek, Andrzej Joachimiak, Zbyszek Otwinowski, S. Moy, Mischa Machius, Pavlina Rezacova

Publikováno v: Molecular Microbiology. 69:895-910

Expression of genes in the gapA operon encoding five enzymes for triose phosphate interconversion in Bacillus subtilis is negatively regulated by the Central glycolytic genes Regulator (CggR). CggR belongs to the large SorC/DeoR family of prokaryotic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88ac76a8eff58963d4dd4fc80628b98b
https://doi.org/10.1111/j.1365-2958.2008.06318.x

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Inorganic Polyhedral Metallacarborane Inhibitors of HIV Protease: A New Approach to Overcoming Antiviral Resistance

Autor: Klára Grantz Šašková, Jan Konvalinka, Jana Václavíková, Jiri Brynda, Jaromír Plešek, Martin Lepšík, Bohumír Grüner, Milan Kozisek, Vladimír Král, Pavlina Rezacova, Petr Cigler, Jana Pokorná, Jindrich Fanfrlík

Publikováno v: Journal of Medicinal Chemistry. 51:4839-4843

HIV protease (PR) is a prime target for rational anti-HIV drug design. We have previously identified icosahedral metallacarboranes as a novel class of nonpeptidic protease inhibitors. Now we show that substituted metallacarboranes are potent and spec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31797c637ddfbe84324480078676ce38
https://doi.org/10.1021/jm8002334

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Ninety-Nine Is Not Enough: Molecular Characterization of Inhibitor-Resistant Human Immunodeficiency Virus Type 1 Protease Mutants with Insertions in the Flap Region

Autor: Milan Kozisek, Jiri Brynda, Ron M. Kagan, Charles A. Boucher, Jan Konvalinka, Pavlina Rezacova, Noortje M van Maarseveen, Dorien de Jong, Klára Grantz Šašková, Monique Nijhuis

Publikováno v: Journal of Virology. 82:5869-5878

While the selection of amino acid insertions in human immunodeficiency virus (HIV) reverse transcriptase (RT) is a known mechanism of resistance against RT inhibitors, very few reports on the selection of insertions in the protease (PR) coding region

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31f815ae4270face4f5e6c5481630ff5
https://doi.org/10.1128/jvi.02325-07

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Tetraphenylporphyrin-cobalt(III) Bis(1,2-dicarbollide) Conjugates: From the Solution Characteristics to Inhibition of HIV Protease

Autor: Petr Cigler, Kamil Lang, Karel Procházka, Pavel Janda, Kral, Zdeněk Zelinger, Pavel Kubát, Matejícek P, Milan Kozisek

Publikováno v: The Journal of Physical Chemistry B. 111:4539-4546

Tetraphenylporphyrin conjugates with one (PB1) and four (PB4) cobalt(III) bis(1,2-dicarbollide) substituents were synthesized and the physicochemical and photophysical properties as well as inhibition of HIV-1 protease were described. In methanol, bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72d76fdaae7b03a22824da733b2e01d8
https://doi.org/10.1021/jp066494p

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Structure-activity study of new inhibitors of human betaine-homocysteine S-methyltransferase

Autor: Milos Budesínský, Vaclav Vanek, Ivona Hančlová, Markos Koutmos, Miloslav Sanda, Ivan Rosenberg, Jiri Brynda, Jana Mládková, Petra Kabeleová, Timothy A. Garrow, Jiri Jiracek, Milan Kozisek

Publikováno v: Journal of medicinal chemistry. 52(12)

Betaine-homocysteine S-methyltransferase (BHMT) catalyzes the transfer of a methyl group from betaine to l-homocysteine, yielding dimethylglycine and l-methionine. In this study, we prepared a new series of BHMT inhibitors. The inhibitors were design

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d0f22e380dc5336ea6cebabbdf54ba3
https://pubmed.ncbi.nlm.nih.gov/19534555

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Stabilization of antibody structure upon association to a human carbonic anhydrase IX epitope studied by X-ray crystallography, microcalorimetry, and molecular dynamics simulations

Autor: R Collard, Jiří Brynda, Milan Fábry, Pavlina Rezacova, Juraj Sedlacek, P. Mader, M. Horejsi, Kral, L Rulisek, Milan Kozisek, J. Zavada

Publikováno v: Proteins. 71(3)

Specific antibodies interfere with the function of human tumor-associated carbonic anhydrase IX (CA IX), and show potential as tools for anticancer interventions. In this work, a correlation between structural elements and thermodynamic parameters of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::107ae4a785e1dbfd88dcfcaf92399f59
https://pubmed.ncbi.nlm.nih.gov/18041760

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