Search Results - "Leung, Eleanor"
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The identification of new metallo-β-lactamase inhibitor leads from fragment-based screening
Published in Bioorganic & medicinal chemistry letters (01-06-2011)“…The emergence of metallo-β-lactamases (MBLs) capable of hydrolysing a broad spectrum of β-lactam antibiotics is particularly concerning for the future…”
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Applications of 19F-NMR in Fragment-Based Drug Discovery
Published in Molecules (Basel, Switzerland) (16-07-2016)“…19 F-NMR has proved to be a valuable tool in fragment-based drug discovery. Its applications include screening libraries of fluorinated fragments, assessing…”
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Promiscuous 2‑Aminothiazoles (PrATs): A Frequent Hitting Scaffold
Published in Journal of medicinal chemistry (12-02-2015)“…We have identified a class of molecules, known as 2-aminothiazoles (2-ATs), as frequent-hitting fragments in biophysical binding assays. This was exemplified…”
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Applications of (19)F-NMR in Fragment-Based Drug Discovery
Published in Molecules (Basel, Switzerland) (16-07-2016)“…(19)F-NMR has proved to be a valuable tool in fragment-based drug discovery. Its applications include screening libraries of fluorinated fragments, assessing…”
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5
Design, Synthesis, and Characterization of Cyclic Peptidomimetics of the Inducible Nitric Oxide Synthase Binding Epitope That Disrupt the Protein–Protein Interaction Involving SPRY Domain-Containing Suppressor of Cytokine Signaling Box Protein (SPSB) 2 and Inducible Nitric Oxide Synthase
Published in Journal of medicinal chemistry (23-06-2016)“…SPRY domain-containing suppressor of cytokine signaling box protein (SPSB) 2-deficient macrophages have been found to exhibit prolonged expression of inducible…”
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Fragment-based and structure-guided discovery of perforin inhibitors
Published in European journal of medicinal chemistry (05-12-2023)“…Perforin is a pore-forming protein whose normal function enables cytotoxic T and natural killer (NK) cells to kill virus-infected and transformed cells…”
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A Potent Cyclic Peptide Targeting SPSB2 Protein as a Potential Anti-infective Agent
Published in Journal of medicinal chemistry (28-08-2014)“…The protein SPSB2 mediates proteosomal degradation of inducible nitric oxide synthase (iNOS). Inhibitors of SPSB2–iNOS interaction may prolong the lifetime of…”
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Expression and isotopic labelling of the potassium channel blocker ShK toxin as a thioredoxin fusion protein in bacteria
Published in Toxicon (Oxford) (01-10-2012)“…The polypeptide toxin ShK is a potent blocker of Kv1.3 potassium channels, which play a crucial role in the activation of human effector memory T-cells (TEM)…”
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The Single Disulfide-Directed β‑Hairpin Fold. Dynamics, Stability, and Engineering
Published in Biochemistry (Easton) (16-05-2017)“…Grafting bioactive peptide sequences onto small cysteine-rich scaffolds is a promising strategy for enhancing their stability and value as novel peptide-based…”
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A Cyclic Peptide Inhibitor of the iNOS–SPSB Protein–Protein Interaction as a Potential Anti-Infective Agent
Published in ACS chemical biology (19-10-2018)“…SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4 interact with inducible nitric oxide synthase (iNOS), causing the iNOS to be…”
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Structure and Functional Characterization of the Conserved JAK Interaction Region in the Intrinsically Disordered N‑Terminus of SOCS5
Published in Biochemistry (Easton) (04-08-2015)“…SOCS5 can negatively regulate both JAK/STAT and EGF-receptor pathways and has therefore been implicated in regulating both the immune response and…”
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Conformational Changes in a Plant Ketol-Acid Reductoisomerase upon Mg2+ and NADPH Binding as Revealed by Two Crystal Structures
Published in Journal of molecular biology (29-05-2009)“…Ketol-acid reductoisomerase (KARI; EC 1.1.1.86) is an enzyme in the branched-chain amino acid biosynthesis pathway where it catalyzes the conversion of…”
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Structural Basis for Ca2+-mediated Interaction of the Perforin C2 Domain with Lipid Membranes
Published in The Journal of biological chemistry (16-10-2015)“…Natural killer cells and cytotoxic T-lymphocytes deploy perforin and granzymes to kill infected host cells. Perforin, secreted by immune cells, binds target…”
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Structure and Function Characterization of the a1a2 Motifs of Streptococcus pyogenes M Protein in Human Plasminogen Binding
Published in Journal of molecular biology (06-09-2019)“…Plasminogen (Plg)-binding M protein (PAM) is a group A streptococcal cell surface receptor that is crucial for bacterial virulence. Previous studies revealed…”
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Redox‐stable cyclic peptide inhibitors of the SPSB2–iNOS interaction
Published in FEBS letters (01-03-2016)“…SPSB2 mediates the proteasomal degradation of iNOS. Inhibitors of SPSB2–iNOS interaction are expected to prolong iNOS lifetime and thereby enhance killing of…”
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The neoepitope of the complement C5b-9 Membrane Attack Complex is formed by proximity of adjacent ancillary regions of C9
Published in Communications biology (13-01-2023)“…The Membrane Attack Complex (MAC) is responsible for forming large β-barrel channels in the membranes of pathogens, such as gram-negative bacteria. Off-target…”
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Identification and characterization of an unusual metallo-β-lactamase from Serratia proteamaculans
Published in Journal of biological inorganic chemistry (01-10-2013)“…Metallo-β-lactamases (MBLs) are a family of metalloenzymes that are capable of hydrolyzing β-lactam antibiotics and are an important means by which bacterial…”
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Structure and activity of contryphan-Vc2: Importance of the d-amino acid residue
Published in Toxicon (Oxford) (01-04-2017)“…In natural proteins and peptides, amino acids exist almost invariably as l-isomers. There are, however, several examples of naturally-occurring peptides…”
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Defining the interaction of perforin with calcium and the phospholipid membrane
Published in Biochemical journal (15-12-2013)“…Following its secretion from cytotoxic lymphocytes into the immune synapse, perforin binds to target cell membranes through its Ca(2+)-dependent C2 domain…”
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Randomized Trial of Dose-Dense Versus Conventionally Scheduled and Sequential Versus Concurrent Combination Chemotherapy as Postoperative Adjuvant Treatment of Node-Positive Primary Breast Cancer: First Report of Intergroup Trial C9741/Cancer and Leukemia Group B Trial 9741
Published in Journal of clinical oncology (15-04-2003)“…Using a 2 x 2 factorial design, we studied the adjuvant chemotherapy of women with axillary node-positive breast cancer to compare sequential doxorubicin (A),…”
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