Search Results - "Hawkins, Alastair R."
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1
Glycan complexity dictates microbial resource allocation in the large intestine
Published in Nature communications (26-06-2015)“…The structure of the human gut microbiota is controlled primarily through the degradation of complex dietary carbohydrates, but the extent to which…”
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2
Quinate-based ligands for irreversible inactivation of the bacterial virulence factor DHQ1 enzyme-A molecular insight
Published in Frontiers in molecular biosciences (24-01-2023)“…Irreversible inhibition of the enzyme type I dehydroquinase (DHQ1), a promising target for anti-virulence drug development, has been explored by enhancing the…”
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3
Mechanistic insight into the reaction catalysed by bacterial type II dehydroquinases
Published in Biochemical journal (15-03-2014)“…DHQ2 (type II dehydroquinase), which is an essential enzyme in Helicobacter pylori and Mycobacterium tuberculosis and does not have any counterpart in humans,…”
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4
Insights into substrate binding and catalysis in bacterial type I dehydroquinase
Published in Biochemical journal (15-09-2014)“…Structural, biochemical and computational studies to study substrate binding and the role of the conserved residues of the DHQ1 (type I dehydroquinase) enzyme…”
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5
GTP Cyclohydrolase II Structure and Mechanism
Published in The Journal of biological chemistry (04-11-2005)“…GTP cyclohydrolase II converts GTP to 2,5-diamino-6-β-ribosyl-4(3H)-pyrimidinone 5′-phosphate, formate and pyrophosphate, the first step in riboflavin…”
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6
The Affinity of a Major Ca2+ Binding Site on GRP78 Is Differentially Enhanced by ADP and ATP
Published in The Journal of biological chemistry (31-03-2006)“…GRP78 is a major protein regulated by the mammalian endoplasmic reticulum stress response, and up-regulation has been shown to be important in protecting cells…”
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7
2-Substituted-3-Dehydroquinic Acids as Potent Competitive Inhibitors of Type II Dehydroquinase
Published in ChemMedChem (07-12-2009)“…Potential antibiotics: The substitution of either the pro‐R or pro‐S hydrogen of the 3‐dehydroquinic acid, the natural substrate of type II dehydroquinase, by…”
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Structure-Based Design, Synthesis, and Biological Evaluation of Inhibitors of Mycobacterium tuberculosis Type II Dehydroquinase
Published in Journal of medicinal chemistry (28-07-2005)“…The syntheses by Suzuki cross-coupling of 12 5-aryl analogues of the known inhibitor (1R,3R,4R)-1,3,4-trihydroxycyclohex-5-en-1-carboxylic acid are reported…”
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9
The Negative Transcriptional Regulator NmrA Discriminates between Oxidized and Reduced Dinucleotides
Published in The Journal of biological chemistry (22-08-2003)“…NmrA, a transcription repressor involved in the regulation of nitrogen metabolism in Aspergillus nidulans,is a member of the short-chain dehydrogenase…”
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10
Crystal Structure of SANOS, a Bacterial Nitric Oxide Synthase Oxygenase Protein from Staphylococcus aureus
Published in Structure (London) (01-12-2002)“…Prokaryotic genes related to the oxygenase domain of mammalian nitric oxide synthases (NOSs) have recently been identified. Although they catalyze the same…”
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11
Competitive Inhibitors of Helicobacter pylori Type II Dehydroquinase: Synthesis, Biological Evaluation, and NMR Studies
Published in ChemMedChem (19-05-2008)“…Several 3‐heteroaryl analogs of the known dehydroquinase inhibitor (1R,4R,5R)‐1,4,5‐trihydroxy‐2‐cyclohexene‐1‐carboxylic acid (4) were synthesized and tested…”
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12
Structure of dehydroquinate synthase reveals an active site capable of multistep catalysis
Published in Nature (London) (16-07-1998)“…Dehydroquinate synthase (DHQS) has long been regarded as a catalytic marvel because of its ability to perform several consecutive chemical reactions in one…”
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13
Self‐Immolation of a Bacterial Dehydratase Enzyme by its Epoxide Product
Published in Chemistry : a European journal (26-06-2020)“…Disabling the bacterial capacity to cause infection is an innovative approach that has attracted significant attention to fight against superbugs. A relevant…”
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14
Crystal structure of NucB, a biofilm-degrading endonuclease
Published in Nucleic acids research (09-01-2018)“…Abstract Bacterial biofilms are a complex architecture of cells that grow on moist interfaces, and are held together by a molecular glue of extracellular…”
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15
Mycobacterium tuberculosis Shikimate Kinase Inhibitors: Design and Simulation Studies of the Catalytic Turnover
Published in Journal of the American Chemical Society (21-08-2013)“…Shikimate kinase (SK) is an essential enzyme in several pathogenic bacteria and does not have any counterpart in human cells, thus making it an attractive…”
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Matriptase Induction of Metalloproteinase‐Dependent Aggrecanolysis In Vitro and In Vivo: Promotion of Osteoarthritic Cartilage Damage by Multiple Mechanisms
Published in Arthritis & rheumatology (Hoboken, N.J.) (01-08-2017)“…Objective To assess the ability of matriptase, a type II transmembrane serine proteinase, to promote aggrecan loss from the cartilage of patients with…”
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Nanomolar Competitive Inhibitors of Mycobacterium tuberculosis and Streptomyces coelicolor Type II Dehydroquinase
Published in ChemMedChem (12-02-2007)“…Isomeric nitrophenyl and heterocyclic analogues of the known inhibitor (1S,3R,4R)‐1,3,4‐trihydroxy‐5‐cyclohexene‐1‐carboxylic acid have been synthesized and…”
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18
Freezing the Dynamic Gap for Selectivity: Motion-Based Design of Inhibitors of the Shikimate Kinase Enzyme
Published in Chemistry : a European journal (12-12-2016)“…Shikimate kinase (SK), the fifth enzyme of the aromatic amino acid biosynthesis, is a recognized target for antibiotic drug discovery. The potential of the…”
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Frontispiece: Freezing the Dynamic Gap for Selectivity: Motion-Based Design of Inhibitors of the Shikimate Kinase Enzyme
Published in Chemistry : a European journal (12-12-2016)“…Inhibitors Enzymes are “dynamic” systems that are able to adopt diverse conformations during catalysis—an open conformation (OFF) for product release and a…”
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Targeting the Motion of Shikimate Kinase: Development of Competitive Inhibitors that Stabilize an Inactive Open Conformation of the Enzyme
Published in Journal of medicinal chemistry (09-06-2016)“…The large conformational changes observed by Molecular Dynamics simulation studies on the product release in the LID and shikimic acid binding (SB) domains of…”
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