Search Results - "Leung, Ivanhoe"
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Protein-Directed Dynamic Combinatorial Chemistry: A Guide to Protein Ligand and Inhibitor Discovery
Published in Molecules (Basel, Switzerland) (16-07-2016)“…Protein-directed dynamic combinatorial chemistry is an emerging technique for efficient discovery of novel chemical structures for binding to a target protein…”
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Substrate specificity of polyphenol oxidase
Published in Critical reviews in biochemistry and molecular biology (03-05-2020)“…The ubiquitous type-3 copper enzyme polyphenol oxidase (PPO) has found itself the subject of profound inhibitor research due to its role in fruit and vegetable…”
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Phosphatidylcholine-Specific Phospholipase C as a Promising Drug Target
Published in Molecules (Basel, Switzerland) (25-07-2023)“…Phosphatidylcholine-specific phospholipase C (PC-PLC) is an enzyme that catalyzes the formation of the important secondary messengers phosphocholine and…”
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MCR-1: a promising target for structure-based design of inhibitors to tackle polymyxin resistance
Published in Drug discovery today (01-01-2019)“…•MCR-1 is a phosphoethanolamine transferase that causes polymyxin resistance, an alarming global antibiotic resistance threat.•Zinc ions are critical for MCR-1…”
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Characterisation and optimisation of a novel laccase from Sulfitobacter indolifex for the decolourisation of organic dyes
Published in International journal of biological macromolecules (01-11-2021)“…Laccases are multi‑copper oxidases that possess the potential for industrial wastewater treatments. In this study, a putative laccase from Sulfitobacter…”
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Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding
Published in Bioorganic & medicinal chemistry letters (15-04-2021)“…[Display omitted] Heat shock protein 90 (Hsp90) is an essential molecular chaperone that performs vital stress-related and housekeeping functions in cells and…”
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Synthesis of the Azepinobisindole Alkaloid Iheyamine A Enabled by a Cross-Mannich Reaction
Published in Organic letters (21-10-2016)“…The total synthesis of the azepinobisindole alkaloid iheyamine A is described. The successful strategy hinged on an intermolecular cross-Mannich reaction…”
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The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases
Published in EMBO reports (01-05-2011)“…Mutations in isocitrate dehydrogenases (IDHs) have a gain‐of‐function effect leading to R (−)‐2‐hydroxyglutarate ( R‐ 2HG) accumulation. By using biochemical,…”
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A Critical Update on the Synthesis of Carboxylated Polymers of Intrinsic Microporosity (C-PIMs)
Published in Macromolecules (11-04-2017)Get full text
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Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials
Published in Chemical science (Cambridge) (2017)“…Inhibition of the human 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (human PHD1-3) causes upregulation of HIF, thus…”
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Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain
Published in PloS one (06-07-2015)“…As part of the cellular adaptation to limiting oxygen availability in animals, the expression of a large set of genes is activated by the upregulation of the…”
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Targeting mRNA translation in Parkinson’s disease
Published in Drug discovery today (01-06-2019)“…[Display omitted] •Parkinson’s disease (PD) is one of the most common neurodegenerative disorders.•Mutations in the genes that are involved in translation are…”
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Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases
Published in Nature communications (26-08-2016)“…The response to hypoxia in animals involves the expression of multiple genes regulated by the αβ-hypoxia-inducible transcription factors (HIFs). The…”
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Novel Thermophilic Bacterial Laccase for the Degradation of Aromatic Organic Pollutants
Published in Frontiers in chemistry (20-10-2021)“…We identified a putative laccase from the thermophilic bacterium . The putative laccase was produced recombinantly and its ability to catalyse the degradation…”
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Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors
Published in Journal of medicinal chemistry (25-11-2021)“…FTO catalyzes the Fe(II) and 2-oxoglutarate (2OG)-dependent modification of nucleic acids, including the demethylation of N 6-methyladenosine (m6A) in mRNA…”
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An investigation into the effect of ribosomal protein S15 phosphorylation on its intermolecular interactions by using phosphomimetic mutant
Published in Chemical communications (Cambridge, England) (21-07-2020)“…An investigation using recombinant ribosomal proteins and synthetic peptide models was conducted to uncover the effect of the introduction of a negative charge…”
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Assays to Study Hypoxia-Inducible Factor Prolyl Hydroxylase Domain 2 (PHD2), a Key Human Oxygen Sensing Protein
Published in Methods in molecular biology (Clifton, N.J.) (2023)“…Molecular oxygen is essential for all multicellular life forms. In humans, the hypoxia-inducible factor (HIF) prolyl hydroxylase domain-containing enzymes…”
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Acetyl-CoA-mediated activation of Mycobacterium tuberculosis isocitrate lyase 2
Published in Nature communications (11-10-2019)“…Isocitrate lyase is important for lipid utilisation by Mycobacterium tuberculosis but its ICL2 isoform is poorly understood. Here we report that binding of the…”
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A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold
Published in Molecules (Basel, Switzerland) (26-09-2018)“…Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that mends topoisomerase 1-mediated DNA damage. Tdp1 is a current inhibition target for the…”
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Targeting isocitrate lyase for the treatment of latent tuberculosis
Published in Drug discovery today (01-07-2017)“…•Isocitrate lyase (ICL) is essential to growth and survival of Mycobacterium tuberculosis (Mtb).•ICL is involved in Mtb glyoxylate and methylisocitrate cycles,…”
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