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  1. Akpunarlieva S, Weidt S, Lamasudin D, Naula C, Henderson D, Barrett M, et al.
    J Proteomics, 2017 02 23;155:85-98.
    PMID: 28040509 DOI: 10.1016/j.jprot.2016.12.009
    Leishmania parasites multiply and develop in the gut of a sand fly vector in order to be transmitted to a vertebrate host. During this process they encounter and exploit various nutrients, including sugars, and amino and fatty acids. We have previously generated a mutant Leishmania line that is deficient in glucose transport and which displays some biologically important phenotypic changes such as reduced growth in axenic culture, reduced biosynthesis of hexose-containing virulence factors, increased sensitivity to oxidative stress, and dramatically reduced parasite burden in both insect vector and macrophage host cells. Here we report the generation and integration of proteomic and metabolomic approaches to identify molecular changes that may explain these phenotypes. Our data suggest changes in pathways of glycoconjugate production and redox homeostasis, which likely represent adaptations to the loss of sugar uptake capacity and explain the reduced virulence of this mutant in sand flies and mammals. Our data contribute to understanding the mechanisms of metabolic adaptation in Leishmania and illustrate the power of integrated proteomic and metabolomic approaches to relate biochemistry to phenotype.

    BIOLOGICAL SIGNIFICANCE: This paper reports the application of comparative proteomic and metabolomic approaches to reveal the molecular basis for important phenotypic changes Leishmania parasites that are deficient in glucose uptake. Leishmania cause a very significant disease burden across the world and there are few effective drugs available for control. This work shows that proteomics and metabolomics can produce complementary data that advance understanding of parasite metabolism and highlight potential new targets for chemotherapy.

    Matched MeSH terms: Leishmania mexicana/metabolism*
  2. Fazia Adyani Ahmad Fuad, Houston Douglas R, Michels Paul AM, Fothergill-gilmore Linda A, Walkinshaw Malcolm D
    Sains Malaysiana, 2016;45:1113-1120.
    Cofactor-independent phosphoglycerate mutase has been proposed as a therapeutic target for the treatment of
    trypanosomatid diseases. In this paper, we report the identification of compounds that could potentially be developed as
    selective inhibitors of cofactor-independent phosphoglycerate mutase from Leishmania mexicana (LmiPGAM). Virtual
    screening was used in this search, as well as compounds identified by high-throughput screening. A ligand-based virtual
    screen programme, ultra fast shape recognition with atom types (UFSRAT), was used to screen for compounds resembling
    the substrate/product, before a structure-based approach was applied using AutoDock 4 and AutoDock Vina in a consensus
    docking scheme. In this way eight selected compounds were identified. In addition, three compounds from the Library of
    Pharmacologically Active Compounds (LOPAC) were selected from the published results of high-throughput screening of
    this library. The inhibitory effects of these compounds were tested at a fixed concentration of 1 mM. The results showed
    that seven compounds inhibited LmiPGAM activity and of these, two compounds (one each from high-throughput and
    virtual screening) showed substantial inhibition (i.e. 14% and 49% remaining activity, respectively). Taken together, the
    findings from this study indicate that these compounds have potential as novel inhibitors that specifically target LmiPGAM.
    Matched MeSH terms: Leishmania mexicana
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