Now showing items 1-20 of 22

  • Advanced model compounds for understanding acid catalyzed lignin depolymerization: identification of renewable aromatics and a lignin-derived solvent 

    Lahive, Ciaran; Deuss, Peter J.; Lancefield, Christopher Stuart; Sun, Zhuohua; Cordes, David B.; Young, Claire M.; Tran, Fanny; Slawin, Alexandra M. Z.; de Vries, Johannes G.; Kamer, Paul C. J.; Westwood, Nicholas J.; Barta, Katalin (2016-07-20) - Journal article
    The development of fundamentally new approaches for lignin depolymerization is challenged by the complexity of this aromatic biopolymer. While overly simplified model compounds often lack relevance to the chemistry of ...
  • Autophagic flux blockage by accumulation of weakly basic tenovins leads to elimination of B-Raf mutant tumour cells that survive vemurafenib 

    Ladds, Marcus J. G. W.; Pastor-Fernández, Andrés; Popova, Gergana; van Leeuwen, Ingeborg M. M.; Eng, Kai Er; Drummond, Catherine J.; Johansson, Lars; Svensson, Richard; Westwood, Nicholas J.; McCarthy, Anna R.; Tholander, Fredrik; Popa, Mihaela; Lane, David P.; McCormack, Emmet; McInerney, Gerald M.; Bhatia, Ravi; Laín, Sonia (2018-04-23) - Journal article
    Tenovin-6 is the most studied member of a family of small molecules with antitumour activity in vivo. Previously, it has been determined that part of the effects of tenovin-6 associate with its ability to inhibit SirT1 and ...
  • A DHODH inhibitor increases p53 synthesis and enhances tumor cell killing by p53 degradation blockage 

    Ladds, Marcus J.G.W.; van Leeuwen, Ingeborg M.M.; Drummond, Catherine J.; Chu, Su; Healy, Alan R.; Popova, Gergana; Pastor-Fernández, Andrés; Mollick, Tanzina; Darekar, Suhas; Sedimbi, Saikiran K.; Nekulova, Marta; Sachweh, Marijke C.C.; Campbell, Johanna; Higgins, Maureen; Tuck, Chloe; Popa, Mihaela; Safont, Mireia Mayoral; Gelebart, Pascal; Fandalyuk, Zinayida; Thompson, Alastair M.; Svensson, Richard; Gustavsson, Anna-Lena; Johansson, Lars; Färnegårdh, Katarina; Yngve, Ulrika; Saleh, Aljona; Haraldsson, Martin; D'Hollander, Agathe C. A.; Franco, Marcela; Zhao, Yan; Håkansson, Maria; Walse, Björn; Larsson, Karin; Peat, Emma M.; Pelechano, Vicent; Lunec, John; Vojtesek, Borivoj; Carmena, Mar; Earnshaw, William C.; McCarthy, Anna R.; Westwood, Nicholas J.; Arsenian-Henriksson, Marie; Lane, David P.; Bhatia, Ravi; McCormack, Emmet; Laín, Sonia (2018-03-16) - Journal article
    The development of non-genotoxic therapies that activate wild-type p53 in tumors is of great interest since the discovery of p53 as a tumor suppressor. Here we report the identification of over 100 small-molecules activating ...
  • Discovery and validation of SIRT2 inhibitors based on tenovin-6 : use of a 1H-NMR method to assess deacetylase activity 

    Pirrie, Lisa; McCarthy, Anna R.; Major, Louise L.; Morkunaite, Vaida; Zubriene, Asta; Matulis, Daumantas; Lain, Sonia; Lebl, Tomas; Westwood, Nicholas J. (2012-10) - Journal article
    The search for potent and selective sirtuin inhibitors continues as chemical tools of this type are of use in helping to assign the function of this interesting class of deacetylases. Here we describe SAR studies starting ...
  • Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator 

    Lain, Sonia; Hollick, Jonathan J.; Campbell, Johanna; Staples, Oliver D.; Higgins, Maureen; Aoubala, Mustapha; McCarthy, Anna; Appleyard, Virginia; Murray, Karen E.; Baker, Lee; Thompson, Alastair; Mathers, Joanne; Holland, Stephen J.; Stark, Michael J. R.; Pass, Georgia; Woods, Julie; Lane, David P.; Westwood, Nicholas J. (2008-05-06) - Journal article
    We have carried out a cell-based screen aimed at discovering small molecules that activate p53 and have the potential to decrease tumor growth. Here, we describe one of our hit compounds, tenovin-1, along with a more ...
  • Dysregulation of autophagy in chronic lymphocytic leukemia with the small-molecule Sirtuin inhibitor Tenovin-6 

    MacCallum, Stephanie F.; Groves, Michael J.; James, John; Murray, Karen; Appleyard, Virginia; Prescott, Alan R.; Drbal, Abed A.; Nicolaou, Anna; Cunningham, Joan; Haydock, Sally; Ganley, Ian G.; Westwood, Nicholas J.; Coates, Philip J.; Lain, Sonia; Tauro, Sudhir (2013-02-14) - Journal article
    Tenovin-6 (Tnv-6) is a bioactive small molecule with anti-neoplastic activity. Inhibition of the Sirtuin class of protein deacetylases with activation of p53 function is associated with the pro-apoptotic effects of Tnv-6 ...
  • Efficient genome engineering of Toxoplasma gondii using CRISPR/Cas9 

    Sidik, Saima M.; Hackett, Caroline G.; Tran, Fanny; Westwood, Nicholas J.; Lourido, Sebastian (2014-06-27) - Journal article
    Toxoplasma gondii is a parasite of humans and animals, and a model for other apicomplexans including Plasmodium spp., the causative agents of malaria. Despite many advances, manipulating the T. gondii genome remains labor ...
  • Electronic and bite angle effects in catalytic C-O bond cleavage of a lignin model compound using ruthenium xantphos complexes 

    Shaw, Luke; Somisara, D. M. Upulani K.; How, Rebecca C.; Westwood, Nicholas J.; Bruijnincx, Pieter C. A.; Weckhuysen, Bert M.; Kamer, Paul C. J. (2017-02-07) - Journal article
    Bite angle and electronic effects on the ruthenium-diphosphine catalysed ether bond cleavage of the lignin β-O-4 model compound 2-phenoxy-1-phenethanol were tested. Enhanced conversion of the substrate was observed with ...
  • Identification of TgCBAP, a novel cytoskeletal protein that localizes to three distinct subcompartments of the toxoplasma gondii pellicle 

    Tilley, Lucas D.; Krishnamurthy, Shruthi; Westwood, Nicholas J.; Ward, Gary E. (2014-06-02) - Journal article
    The cytoskeletons of Toxoplasma gondii and related apicomplexan parasites are highly polarized, with apical and basal regions comprised of distinct protein complexes. Components of these complexes are known to play important ...
  • Investigation of the chemocatalytic and biocatalytic valorization of a range of different lignin preparations : the importance of β-O-4 content 

    Lancefield, Christopher S.; Rashid, Goran M. M.; Bouxin, Florent; Wasak, Agata; Tu, Wei-Chien; Hallett, Jason P.; Zein, Sharif; Rodríguez, Jaime; Jackson, S. David; Westwood, Nicholas J.; Bugg, Timothy D. H. (2016-12-05) - Journal article
    A set of seven different lignin preparations was generated from a range of organosolv (acidic, alkaline, ammonia-treated and dioxane-based), ionic liquid, autohydrolysis and Kraft pretreatments of lignocelluloses. Each ...
  • Iso-seco-tanapartholides : isolation, synthesis and biological evaluation 

    Makiyi, Edward F.; Frade, Raquel F. M.; Lebl, Tomas; Jaffray, Ellis G.; Cobb, Susan E.; Harvey, Alan L.; Slawin, Alexandra M. Z.; Hay, Ronald T.; Westwood, Nicholas J. (2009-11) - Journal article
    The isolation, identification and total synthesis of two plant-derived inhibitors of the NF-kappa B signaling pathway from the iso-seco-tanapartholide family of natural products is described. A key step in the efficient ...
  • Isothiourea-catalysed acylative kinetic resolution of aryl-alkenyl (sp2 vs. sp2) substituted secondary alcohols 

    Musolino, Stefania F.; Ojo, O. Stephen; Westwood, Nicholas J.; Taylor, James E.; Smith, Andrew D. (2016-12-23) - Journal article
    The non-enzymatic acylative kinetic resolution of challenging aryl–alkenyl (sp2 vs. sp2) substituted secondary alcohols is described, with effective enantiodiscrimination achieved using the isothiourea organocatalyst ...
  • A modular approach to triazole-containing chemical inducers of dimerisation for yeast three-hybrid screening 

    Tran, Fanny; Odell, Anahi V.; Ward, Gary E.; Westwood, Nicholas J. (2013-09-23) - Journal article
    The yeast three-hybrid (Y3H) approach shows considerable promise for the unbiased identification of novel small molecule-protein interactions. In recent years, it has been successfully used to link a number of bioactive ...
  • Pre-treatment of lignocellulosic feedstocks using biorenewable alcohols : towards complete biomass valorisation 

    Lancefield, Christopher S.; Panovic, Isabella; Deuss, Peter J.; Barta, Katalin; Westwood, Nicholas J. (2017-01-07) - Journal article
    Here, we report on the ability of the biomass derived solvents ethanol and, in particular, n-butanol to fractionate lignocellulose into its main components. An organosolv system consisting of n-butanol containing 5% water ...
  • A proteomic approach to analyze the aspirin-mediated lysine acetylome 

    Tatham, Michael H.; Cole, Christian; Scullian, Paul; Wilkie, Ross; Westwood, Nicholas J.; Stark, Lesley A.; Hay, Ronald T. (2017-02-01) - Journal article
    Aspirin, or acetylsalicylic acid is widely used to control pain, inflammation and fever. Important to this function is its ability to irreversibly acetylate cyclooxygenases at active site serines. Aspirin has the potential ...
  • A Random Forest model for predicting allosteric and functional sites on proteins 

    Chen, Ava S.-Y.; Westwood, Nicholas J.; Brear, Paul; Rogers, Graeme W.; Mavridis, Lazaros; Mitchell, John B. O. (2016-04-05) - Journal article
    We created a computational method to identify allosteric sites using a machine learning method trained and tested on protein structures containing bound ligand molecules. The Random Forest machine learning approach was ...
  • A small-molecule inhibitor of T. gondii motility induces the posttranslational modification of myosin light chain-1 and inhibits myosin motor activity 

    Heaslip, Aoife T.; Leung, Jacqueline M.; Carey, Kimberly L.; Catti, Federica; Warshaw, David M.; Westwood, Nicholas J.; Ballif, Bryan A.; Ward, Gary E. (2010-01-15) - Journal article
    Toxoplasma gondii is an obligate intracellular parasite that enters cells by a process of active penetration. Host cell penetration and parasite motility are driven by a myosin motor complex consisting of four known proteins: ...
  • Structure-activity relationships of the Human Immunodeficiency Virus Type 1 maturation inhibitor PF-46396 

    Murgatroyd, Christopher; Pirrie, Lisa; Fanny Tran; Smith, Terry K.; Westwood, Nicholas J.; Adamson, Catherine S. (2016-09) - Journal article
    HIV-1 maturation inhibitors are a novel class of antiretroviral compounds, which consist of two structurally distinct chemical classes; betulinic acid derivatives and the pyridone-based compound PF-46396. It is currently ...
  • The synthesis and analysis of lignin-bound Hibbert ketone structures in technical lignins 

    Miles-Barrett, Daniel; Neal, Andrew; Hand, Calum; Montgomery, James; Panovic, Isabella; Ojo, Oluwarotimi Stephen; Lancefield, Christopher Stuart; Cordes, David B.; Slawin, Alexandra M. Z.; Lebl, Tomas; Westwood, Nicholas J. (2016-11-14) - Journal article
    Understanding the structure of technical lignins resulting from acid-catalysed treatment of lignocellulosic biomass is important for their future applications. Here we report an investigation into the fate of lignin under ...
  • Synthesis of hybrid cyclopeptides through enzymatic macrocyclization 

    Oueis, Emilia; Nardone, Brunello; Jaspars, Marcel; Westwood, Nicholas J.; Naismith, James H. (2017-02-02) - Journal article
    Natural products comprise a diverse array of molecules many of which are biologically active. Most natural products derive from combinations of polyketides, peptides, sugars and fatty acid building blocks. Peptidic macrocycles ...