Search Results - "Ferguson, Andrew D."
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Structural Basis of Substrate Methylation and Inhibition of SMYD2
Published in Structure (London) (07-09-2011)“…Protein lysine methyltransferases are important regulators of epigenetic signaling. These enzymes catalyze the transfer of donor methyl groups from…”
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Structural basis of CX-4945 binding to human protein kinase CK2
Published in FEBS letters (03-01-2011)“…Protein kinase CK2 (CK2), a constitutively active serine/threonine kinase, is involved in a variety of roles essential to the maintenance of cellular…”
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Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases
Published in Bioorganic & medicinal chemistry letters (15-07-2012)“…Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The…”
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4
Crystal Structure of Inhibitor-Bound Human 5-Lipoxygenase: Activating Protein
Published in Science (American Association for the Advancement of Science) (27-07-2007)“…Leukotrienes are proinflammatory products of arachidonic acid oxidation by 5-lipoxygenase that have been shown to be involved in respiratory and cardiovascular…”
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NMR Structures of the Selenoproteins Sep15 and SelM Reveal Redox Activity of a New Thioredoxin-like Family
Published in The Journal of biological chemistry (10-02-2006)“…Selenium has significant health benefits, including potent cancer prevention activity and roles in immune function and the male reproductive system…”
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Negamycin induces translational stalling and miscoding by binding to the small subunit head domain of the Escherichia coli ribosome
Published in Proceedings of the National Academy of Sciences - PNAS (18-11-2014)“…Significance The identification of negamycin’s binding site within helix 34 of the small subunit head domain and the elucidation of its mechanism of action…”
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Biochemical Characterization of Human SET and MYND Domain-Containing Protein 2 Methyltransferase
Published in Biochemistry (Easton) (26-07-2011)“…SET and MYND domain-containing protein 2 (SMYD2) is a protein lysine methyltransferase that catalyzes the transfer of methyl groups from S-adenosylmethionine…”
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Structural Basis of Gating by the Outer Membrane Transporter FecA
Published in Science (American Association for the Advancement of Science) (01-03-2002)“…Siderophore-mediated acquisition systems facilitate iron uptake. We present the crystallographic structure of the integral outer membrane receptor FecA from…”
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Phosphorylation of Glutamine Synthetase on Threonine 301 Contributes to Its Inactivation During Epilepsy
Published in Frontiers in molecular neuroscience (21-05-2019)“…The astrocyte-specific enzyme glutamine synthetase (GS), which catalyzes the amidation of glutamate to glutamine, plays an essential role in supporting…”
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Signal transduction pathway of TonB-dependent transporters
Published in Proceedings of the National Academy of Sciences - PNAS (09-01-2007)“…Transcription of the ferric citrate import system is regulated by ferric citrate binding to the outer membrane transporter FecA. A signal indicating…”
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The ER protein folding sensor UDP-glucose glycoprotein-glucosyltransferase modifies substrates distant to local changes in glycoprotein conformation
Published in Nature structural & molecular biology (01-02-2004)“…We present in vitro data that explain the recognition mechanism of misfolded glycoproteins by UDP-glucose glycoprotein-glucosyltransferase (UGGT). The…”
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A Novel Cysteine-rich Domain of Sep15 Mediates the Interaction with UDP-glucose:Glycoprotein Glucosyltransferase
Published in The Journal of biological chemistry (11-11-2005)“…Selenium is an essential trace element with potent cancer prevention activity in mammals. The 15-kDa selenoprotein (Sep15) has been implicated in the…”
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13
Discovery of aminopiperidine-based Smac mimetics as IAP antagonists
Published in Bioorganic & medicinal chemistry letters (15-02-2012)“…A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously…”
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A conserved structural motif for lipopolysaccharide recognition by procaryotic and eucaryotic proteins
Published in Structure (London) (15-06-2000)“…Background: Lipopolysaccharide (LPS), a lipoglycan from the outer membrane of Gram-negative bacteria, is an immunomodulatory molecule that stimulates the…”
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15
Structural approaches to obtain kinase selectivity
Published in Trends in pharmacological sciences (Regular ed.) (01-05-2012)“…One of the grand challenges in kinase drug discovery is the design of small-molecule inhibitors with selectivity profiles that will ultimately be efficacious…”
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Analysis of the Substrate Specificity of the SMYD2 Protein Lysine Methyltransferase and Discovery of Novel Non‐Histone Substrates
Published in Chembiochem : a European journal of chemical biology (15-01-2020)“…The SMYD2 protein lysine methyltransferase methylates various histone and non‐histone proteins and is overexpressed in several cancers. Using peptide arrays,…”
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Rational design of a new antibiotic class for drug-resistant infections
Published in Nature (London) (30-09-2021)“…The development of new antibiotics to treat infections caused by drug-resistant Gram-negative pathogens is of paramount importance as antibiotic resistance…”
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Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies
Published in Journal of medicinal chemistry (24-12-2020)“…A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for…”
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Development of a Novel B‑Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6
Published in ACS chemical biology (16-11-2018)“…B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological cancers but high quality chemical probes are necessary to evaluate its…”
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A novel strain of lumpy skin disease virus causes clinical disease in cattle in Hong Kong
Published in Transboundary and emerging diseases (01-07-2022)“…Lumpy skin disease virus (LSDV) is an emerging poxviral pathogen of cattle that is currently spreading throughout Asia. The disease situation is of high…”
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