Search Results - "Kutil, Zsofia"
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One-Atom Substitution Enables Direct and Continuous Monitoring of Histone Deacylase Activity
Published in Biochemistry (Easton) (03-12-2019)“…We developed a one-step direct assay for the determination of histone deacylase (HDAC) activity by substituting the carbonyl oxygen of the acyl moiety with…”
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2
Structure-based molecular modeling in SAR analysis and lead optimization
Published in Computational and structural biotechnology journal (01-01-2021)“…[Display omitted] In silico methods like molecular docking and pharmacophore modeling are established strategies in lead identification. Their successful…”
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3
A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging
Published in Nature communications (15-09-2021)“…Surgery is an efficient way to treat localized prostate cancer (PCa), however, it is challenging to demarcate rapidly and accurately the tumor boundary…”
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4
Predicting Effects of Site-Directed Mutagenesis on Enzyme Kinetics by QM/MM and QM Calculations: A Case of Glutamate Carboxypeptidase II
Published in The journal of physical chemistry. B (13-01-2022)“…Quantum and molecular mechanics (QM/MM) and QM-only (cluster model) modeling techniques represent the two workhorses in mechanistic understanding of enzyme…”
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5
Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome
Published in ACS chemical neuroscience (20-03-2019)“…Disease-modifying therapies are needed for Fragile X Syndrome (FXS), as at present there are no effective treatments or cures. Herein, we report on a…”
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6
Characterization of the class IIa histone deacetylases substrate specificity
Published in The FASEB journal (01-05-2022)“…Class IIa histone deacetylases (HDACs) play critical roles in vertebrate development and physiology, yet direct evidence of their intrinsic deacetylase…”
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7
Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors
Published in ACS omega (26-11-2019)“…Histone deacetylase 11 (HDAC11) preferentially removes fatty acid residues from lysine side chains in a peptide or protein environment. Here, we report the…”
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8
The unraveling of substrate specificity of histone deacetylase 6 domains using acetylome peptide microarrays and peptide libraries
Published in The FASEB journal (01-03-2019)“…ABSTRACT Histone deacetylase 6 (HDAC6) is a multidomain cytosolic hydrolase acting mostly on nonhistone protein substrates. Investigations of the substrate…”
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9
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells
Published in International journal of molecular sciences (01-03-2023)“…Histone deacetylase 6 (HDAC6) is a unique member of the HDAC family of enzymes due to its complex domain organization and cytosolic localization. Experimental…”
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10
Generation and characterization of human U-2 OS cell lines with the CRISPR/Cas9-edited protoporphyrinogen oxidase IX gene
Published in Scientific reports (12-10-2022)“…In humans, disruptions in the heme biosynthetic pathway are associated with various types of porphyrias, including variegate porphyria that results from the…”
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11
Characterization of glutamate carboxypeptidase 2 orthologs in trematodes
Published in Parasites & vectors (20-12-2022)“…Glutamate carboxypeptidase 2 (GCP2) belongs to the M28B metalloprotease subfamily encompassing a variety of zinc-dependent exopeptidases that can be found in…”
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12
Impact of Wines and Wine Constituents on Cyclooxygenase-1, Cyclooxygenase-2, and 5-Lipoxygenase Catalytic Activity
Published in Mediators of Inflammation (01-01-2014)“…Cyclooxygenases and lipoxygenases are proinflammatory enzymes; the former affects platelet aggregation, vasoconstriction, vasodilatation and later the…”
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13
Platelet aggregation and anti-inflammatory effects of garden pea, Desi chickpea and Kabuli chickpea
Published in Acta Poloniae pharmaceutica (01-07-2012)“…Inflammation is the natural body defense mechanism for the removal of injurious agents, necrosed cells and tissues from the body. This study was aimed to…”
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14
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot–Marie–Tooth Type 2A Mouse Model
Published in Journal of medicinal chemistry (22-04-2021)“…Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6…”
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15
Anti-inflammatory Activity of Natural Geranylated Flavonoids: Cyclooxygenase and Lipoxygenase Inhibitory Properties and Proteomic Analysis
Published in Journal of natural products (Washington, D.C.) (28-04-2017)“…Geranyl flavones have been studied as compounds that potentially can be developed as anti-inflammatory agents. A series of natural geranylated flavanones was…”
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Comprehensive Mechanistic View of the Hydrolysis of Oxadiazole-Based Inhibitors by Histone Deacetylase 6 (HDAC6)
Published in ACS chemical biology (21-07-2023)“…Histone deacetylase (HDAC) inhibitors used in the clinic typically contain a hydroxamate zinc-binding group (ZBG). However, more recent work has shown that the…”
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17
Tunnel vision in the drinking water research field – Time for non-targeted analysis implementation?
Published in The Science of the total environment (15-01-2024)“…A plethora of compounds can reach our drinking water and possibly affect human health. Still, mostly notorious pollutants like pesticides and disinfection…”
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18
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models
Published in ACS medicinal chemistry letters (12-10-2017)“…Only a handful of therapies offer significant improvement in the overall survival in cases of melanoma, a cancer whose incidence has continued to rise in the…”
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19
Histone Deacetylase 11 Is a Fatty-Acid Deacylase
Published in ACS chemical biology (16-03-2018)“…Histone deacetylase 11 (HDAC11) is a sole member of the class IV HDAC subfamily with negligible intrinsic deacetylation activity. Here, we report in vitro…”
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20
Natural Compound Cudraflavone B Shows Promising Anti-inflammatory Properties in Vitro
Published in Journal of natural products (Washington, D.C.) (25-04-2011)“…Cudraflavone B (1) is a prenylated flavonoid found in large amounts in the roots of Morus alba, a plant used as a herbal remedy for its reputed…”
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