Search Results - "Chalupská, Dominika"
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Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4‑Kinase IIIβ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology
Published in Journal of medicinal chemistry (12-01-2017)“…Phosphatidylinositol 4-kinase IIIβ (PI4KB) is indispensable for the replication of various positive-sense single stranded RNA viruses, which hijack this…”
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Highly Selective Phosphatidylinositol 4‑Kinase IIIβ Inhibitors and Structural Insight into Their Mode of Action
Published in Journal of medicinal chemistry (14-05-2015)“…Phosphatidylinositol 4-kinase IIIβ is a cellular lipid kinase pivotal to pathogenesis of various RNA viruses. These viruses hijack the enzyme in order to…”
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Rational Design of Highly Potent SARS-CoV‑2 nsp14 Methyltransferase Inhibitors
Published in ACS omega (01-08-2023)“…The search for new drugs against COVID-19 and its causative agent, SARS-CoV-2, is one of the major trends in the current medicinal chemistry. Targeting capping…”
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Structural basis of RNA recognition by the SARS-CoV-2 nucleocapsid phosphoprotein
Published in PLoS pathogens (02-12-2020)“…Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of the coronavirus disease 2019 (COVID-19). SARS-CoV-2 is a single-stranded…”
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PI(4,5)P2 controls plasma membrane PI4P and PS levels via ORP5/8 recruitment to ER–PM contact sites
Published in The Journal of cell biology (07-05-2018)“…Phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) is a critically important regulatory lipid of the plasma membrane (PM); however, little is known about how…”
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Discovery and structural characterization of monkeypox virus methyltransferase VP39 inhibitors reveal similarities to SARS-CoV-2 nsp14 methyltransferase
Published in Nature communications (20-04-2023)“…Monkeypox is a disease with pandemic potential. It is caused by the monkeypox virus (MPXV), a double-stranded DNA virus from the Poxviridae family, that…”
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Structure-based design and modular synthesis of novel PI4K class II inhibitors bearing a 4-aminoquinazoline scaffold
Published in Bioorganic & medicinal chemistry letters (15-11-2022)Get full text
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Design, synthesis and evaluation of novel thieno[2,3d]pyrimidine derivatives as potent and specific RIPK2 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-01-2024)“…In human cells, receptor-interacting protein kinase 2 (RIPK2) is mainly known to mediate downstream enzymatic cascades from the nucleotide-binding…”
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Phosphatidylinositol 4-kinase IIIβ (PI4KB) forms highly flexible heterocomplexes that include ACBD3, 14-3-3, and Rab11 proteins
Published in Scientific reports (24-01-2019)“…Phosphatidylinositol 4-kinase IIIβ (PI4KB) is a key enzyme of the Golgi system because it produces its lipid hallmark - the phosphatidylinositol 4-phosphate…”
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Exploring positions 6 and 7 of a quinazoline-based scaffold leads to changes in selectivity and potency towards RIPK2/3 kinases
Published in European journal of medicinal chemistry (15-11-2023)“…Receptor-interacting protein kinases 2 and 3 (RIPK2 and RIPK3) are considered attractive therapeutic enzyme targets for the treatment of a multitude of…”
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Antiviral Properties of the NSAID Drug Naproxen Targeting the Nucleoprotein of SARS-CoV-2 Coronavirus
Published in Molecules (Basel, Switzerland) (29-04-2021)“…There is an urgent need for specific antiviral treatments directed against SARS-CoV-2 to prevent the most severe forms of COVID-19. By drug repurposing,…”
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Structural insights and in vitro reconstitution of membrane targeting and activation of human PI4KB by the ACBD3 protein
Published in Scientific reports (24-03-2016)“…Phosphatidylinositol 4-kinase beta (PI4KB) is one of four human PI4K enzymes that generate phosphatidylinositol 4-phosphate (PI4P), a minor but essential…”
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Convergent evolution in the mechanisms of ACBD3 recruitment to picornavirus replication sites
Published in PLoS pathogens (05-08-2019)“…Enteroviruses, members of the family of picornaviruses, are the most common viral infectious agents in humans causing a broad spectrum of diseases ranging from…”
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Localization of SARS-CoV-2 Capping Enzymes Revealed by an Antibody against the nsp10 Subunit
Published in Viruses (29-07-2021)“…Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of the coronavirus disease-19 pandemic. One of the key components of the…”
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A large scale high-throughput screen identifies chemical inhibitors of phosphatidylinositol 4-kinase type II alpha[S]
Published in Journal of lipid research (01-03-2019)“…The minor phospholipid, phosphatidylinositol 4-phosphate (PI4P), is emerging as a key regulator of lipid transfer in ER-membrane contact sites. Four different…”
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Adaptation of an L-proline adenylation domain to use 4-propyl-L-proline in the evolution of lincosamide biosynthesis
Published in PloS one (27-12-2013)“…Clinically used lincosamide antibiotic lincomycin incorporates in its structure 4-propyl-L-proline (PPL), an unusual amino acid, while celesticetin, a less…”
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Single-site mutations in the carboxyltransferase domain of plastid acetyl-CoA carboxylase confer resistance to grass-specific herbicides
Published in Proceedings of the National Academy of Sciences - PNAS (27-02-2007)“…Grass weed populations resistant to aryloxyphenoxypropionate (APP) and cyclohexanedione herbicides that inhibit acetyl-CoA carboxylase (ACCase; EC 6.4.1.2)…”
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Norbornane-based nucleoside and nucleotide analogues locked in North conformation
Published in Bioorganic & medicinal chemistry (01-01-2015)“…[Display omitted] We report on the synthesis of novel conformationally locked nucleoside and nucleotide derivatives, which are structurally closely related to…”
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Recombinant yeast screen for new inhibitors of human acetyl-CoA carboxylase 2 identifies potential drugs to treat obesity
Published in Proceedings of the National Academy of Sciences - PNAS (18-05-2010)“…Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism with multiple isozymes often expressed in different eukaryotic cellular compartments…”
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Structural and functional insights in flavivirus NS5 proteins gained by the structure of Ntaya virus polymerase and methyltransferase
Published in Structure (London) (08-08-2024)“…Flaviviruses are single-stranded positive-sense RNA (+RNA) viruses that are responsible for several (re)emerging diseases such as yellow, dengue, or West Nile…”
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