Publications
168 results found
Elvira KS, Leatherbarrow R, Edel JB, et al., 2012, Droplet dispensing in digital microfluidic devices: Assessment of long-term reproducibility, Biomicrofluidics
Bradshaw RT, Aronica PGA, Tate EW, et al., 2012, Mutational Locally Enhanced Sampling (MULES) for quantitative prediction of the effects of mutations at protein-protein interfaces, CHEMICAL SCIENCE, Vol: 3, Pages: 1503-1511, ISSN: 2041-6520
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- Citations: 2
Carr JL, Sejberg JJP, Saab F, et al., 2011, Synthesis of the C19 methyl ether of aspercyclide A via germyl-Stille macrocyclisation and ELISA evaluation of both enantiomers following optical resolution., Org Biomol Chem, Vol: 9, Pages: 6814-6824
Aspercyclide A (1) is a biaryl ether containing 11-membered macrocyclic natural product antagonist of the human IgE-FcεRI protein-protein interaction (PPI); a key interaction in the signal transduction pathway for allergic disorders such as asthma. Herein we report a novel approach to the synthesis of the C19 methyl ether of aspercyclide A, employing a Pd(0)-catalysed, fluorous-tagged alkenylgermane/arylbromide macrocyclisation (germyl-Stille reaction) as the key step, and evaluation of both enantiomers of this compound via ELISA following optical resolution by CSP-HPLC. A crystal structure for germyl hydride 27 is also reported.
Stuart SF, Leatherbarrow RJ, Willison KR, 2011, A Two-step Mechanism for the Folding of Actin by the Yeast Cytosolic Chaperonin, JOURNAL OF BIOLOGICAL CHEMISTRY, Vol: 286, Pages: 178-184
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- Citations: 21
Bradshaw RT, Patel BH, Tate EW, et al., 2010, Comparing experimental and computational alanine scanning techniques for probing a prototypical protein-protein interaction, PROTEIN ENGINEERING DESIGN & SELECTION, Vol: 24, Pages: 197-207, ISSN: 1741-0126
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- Citations: 62
Brannigan JA, Smith BA, Yu Z, et al., 2010, N-Myristoyltransferase from Leishmania donovani: Structural and Functional Characterisation of a Potential Drug Target for Visceral Leishmaniasis, Journal of Molecular Biology, Vol: 396, Pages: 985-999, ISSN: 1089-8638
N-Myristoyltransferase (NMT) catalyses the attachment of the 14-carbon saturated fatty acid, myristate, to the amino-terminal glycine residue of a subset of eukaryotic proteins that function in multiple cellular processes, including vesicular protein trafficking and signal transduction. In these pathways, N-myristoylation facilitates association of substrate proteins with membranes or the hydrophobic domains of other partner peptides. NMT function is essential for viability in all cell types tested to date, demonstrating that this enzyme has potential as a target for drug development. Here, we provide genetic evidence that NMT is likely to be essential for viability in insect stages of the pathogenic protozoan parasite, Leishmania donovani, causative agent of the tropical infectious disease, visceral leishmaniasis. The open reading frame of L. donovaniNMT has been amplified and used to overproduce active recombinant enzyme in Escherichia coli, as demonstrated by gel mobility shift assays of ligand binding and peptide-myristoylation activity in scintillation proximity assays. The purified protein has been crystallized in complex with the non-hydrolysable substrate analogue S-(2-oxo)pentadecyl-CoA, and its structure was solved by molecular replacement at 1.4 Å resolution. The structure has as its defining feature a 14-stranded twisted β-sheet on which helices are packed so as to form an extended and curved substrate-binding groove running across two protein lobes. The fatty acyl-CoA is largely buried in the N-terminal lobe, its binding leading to the loosening of a flap, which in unliganded NMT structures, occludes the protein substrate binding site in the carboxy-terminal lobe. These studies validate L. donovani NMT as a potential target for development of new therapeutic agents against visceral leishmaniasis.
Zunszain PA, Knox SR, Sweeney TR, et al., 2010, Insights into Cleavage Specificity from the Crystal Structure of Foot-and-Mouth Disease Virus 3C Protease Complexed with a Peptide Substrate, JOURNAL OF MOLECULAR BIOLOGY, Vol: 395, Pages: 375-389, ISSN: 0022-2836
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- Citations: 53
So S, Peeva LG, Tate EW, et al., 2010, Membrane enhanced peptide synthesis, CHEMICAL COMMUNICATIONS, Vol: 46, Pages: 2808-2810, ISSN: 1359-7345
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- Citations: 40
So S, Peeva LG, Tate EW, et al., 2010, Organic Solvent Nanofiltration: A New Paradigm in Peptide Synthesis, Org Process Res Dev, Vol: 14, Pages: 1313-1325
Carr JL, Offermann DA, Holdom MD, et al., 2010, Total synthesis of (±)-aspercyclide A and its C19 methyl ether, CHEMICAL COMMUNICATIONS, Vol: 46, Pages: 1824-1826, ISSN: 1359-7345
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- Citations: 23
Thongyoo P, Bonomelli C, Leatherbarrow RJ, et al., 2009, Potent Inhibitors of β-Tryptase and Human Leukocyte Elastase Based on the MCoTI-II Scaffold, JOURNAL OF MEDICINAL CHEMISTRY, Vol: 52, Pages: 6197-6200, ISSN: 0022-2623
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- Citations: 104
Srisa-Art M, Kang D-K, Hong J, et al., 2009, Analysis of Protein-Protein Interactions by Using Droplet-Based Microfluidics, CHEMBIOCHEM, Vol: 10, Pages: 1605-1611, ISSN: 1439-4227
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- Citations: 55
Busch GK, Tate EW, Gaffney PR, et al., 2008, Specific N-terminal protein labelling: use of FMDV 3C pro protease and native chemical ligation, Chem.Commun.(Camb.), Pages: 3369-3371
We report an effective strategy for generating N-terminal cysteinyl proteins by proteolytic cleavage using the enzyme 3C pro, suitable for a wide range of applications via native chemical ligation
Heal WP, Wickramasinghe SR, Leatherbarrow RJ, et al., 2008, N-Myristoyl transferase-mediated protein labelling in vivo, Organic and Biomolecular Chemistry
Bowyer PW, Tate EW, Leatherbarrow RJ, et al., 2008, <i>N</i>-myristoyltransferase:: a prospective drug target for protozoan parasites, CHEMMEDCHEM, Vol: 3, Pages: 402-408, ISSN: 1860-7179
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- Citations: 54
Heal WP, Wickramasinghe SR, Bowyer PW, et al., 2008, Site-specific N-terminal labelling of proteins in vitro and in vivo using N-myristoyl transferase and bioorthogonal ligation chemistry, Chem. Commun.
Thongyoo P, Roque-Rosell N, Leatherbarrow RJ, et al., 2008, Chemical and biomimetic total syntheses of natural and engineered MCoTI cyclotides, ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 6, Pages: 1462-1470, ISSN: 1477-0520
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- Citations: 124
Bowyer PW, Gunaratne RS, Grainger M, et al., 2007, Molecules incorporating a benzothiazole core scaffold inhibit the N-myristoyltransferase of <i>Plasmodium falciparum</i>, BIOCHEMICAL JOURNAL, Vol: 408, Pages: 173-180, ISSN: 0264-6021
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- Citations: 55
Jaulent AM, Fahy AS, Knox SR, et al., 2007, A continuous assay for foot-and-mouth disease virus 3C protease activity, ANALYTICAL BIOCHEMISTRY, Vol: 368, Pages: 130-137, ISSN: 0003-2697
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- Citations: 14
Thongyoo P, Jaulent AM, Tate EW, et al., 2007, Immobilized protease-assisted synthesis of engineered cysteine-knot microproteins, CHEMBIOCHEM, Vol: 8, Pages: 1107-1109, ISSN: 1439-4227
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- Citations: 42
Brauer ABE, McBride JD, Kelly G, et al., 2007, Resisting degradation by human elastase: Commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds, BIOORGANIC & MEDICINAL CHEMISTRY, Vol: 15, Pages: 4618-4628, ISSN: 0968-0896
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- Citations: 4
Curry S, Roque-Rosell N, Sweeney TR, et al., 2007, Structural analysis of foot-and-mouth disease virus 3C protease:: a viable target for antiviral drugs?, BIOCHEMICAL SOCIETY TRANSACTIONS, Vol: 35, Pages: 594-598, ISSN: 0300-5127
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- Citations: 20
Roque-Rosell N, Curry S, Leatherbarrow RJ, 2007, Studies toward a new foot-and-mouth disease antiviral agent, ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, Vol: 233, Pages: 515-515, ISSN: 0065-7727
Sweeney TR, Roque-Rosell N, Birtley JR, et al., 2007, Structural and mutagenic analysis of foot-and-mouth disease virus 3C protease reveals the role of the β-ribbon in proteolysis, JOURNAL OF VIROLOGY, Vol: 81, Pages: 115-124, ISSN: 0022-538X
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- Citations: 73
Sweeney TR, Zunszain PA, Roque-Rosell N, et al., 2007, Structural and mutagenic analysis of foot-and-mouth disease virus 3C protease, Publisher: INT UNION CRYSTALLOGRAPHY, Pages: S26-S26, ISSN: 2053-2733
Curry S, Roque-Rosell N, Zunszain PA, et al., 2007, Foot-and-mouth disease virus 3C protease:: Recent structural and functional insights into an antiviral target, INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY, Vol: 39, Pages: 1-6, ISSN: 1357-2725
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- Citations: 40
Panethymitaki C, Bowyer PW, Price HP, et al., 2006, Characterization and selective inhibition of myristoyl-CoA:protein <i>N</i>-myristoyltransferase from <i>Trypanosoma brucei</i> and <i>Leishmania major</i>, BIOCHEMICAL JOURNAL, Vol: 396, Pages: 277-285, ISSN: 0264-6021
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- Citations: 51
Allen SH, Johns BA, Gudmundsson KS, et al., 2006, Synthesis of C-6 substituted pyrazolol[1,5-α]pyridines with potent activity against herpesviruses, BIOORGANIC & MEDICINAL CHEMISTRY, Vol: 14, Pages: 944-954, ISSN: 0968-0896
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- Citations: 39
Thongyoo P, Tate EW, Leatherbarrow RJ, 2006, Total synthesis of the macrocyclic cysteine-knot microprotein MCoTI-II, Chemical Communications, Vol: 2006, Pages: 2848-2850, ISSN: 1359-7345
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