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Biology subjects

Butler, M. S.

Publications and source records attributed to Butler, M. S..

3 recordsLinked to original sources

FLONE: fully Lorentz network embedding for inferring novel drug targets

MotivationTo predict novel drug targets, graph-based machine learning methods have been widely used to capture the relationships between drug, target, and disease entities in heterogeneous biological networks. However, most of the existing methods cannot explicitly consider disease types when predicting targets. More importantly, drug-disease-target (DDT) networks could exhibit multi-relational hierarchical sub-structures with the information of biological interactive functions, but these methods, especially those based on Euclidean space embedding cannot fully utilize such topology information, which might lead to sub-optimal prediction results. We hypothesized that, by properly importing hyperbolic space embedding specifically for modeling hierarchical DDT networks, graph-based machine learning algorithms could better capture the relationships between aforementioned entities, which ultimately improves the target prediction performance. ResultsTo test our hypothesis, we formulated the drug target prediction problem as a knowledge graph triple completion task explicitly considering disease types. To solve this problem, we proposed FLONE, a novel hyperbolic Lorentz space embedding-based method to capture the hierarchical structural information in the DDT network when inferring drug targets. We evaluated it on two different DDT networks, our experimental results showed that by introducing Lorentz space, one of the isomorphic models of hyperbolic space, FLONE generates more accurate candidate target predictions given the drug and disease than the Euclidean translation-based counterparts, which supports our hypothesis. Beyond these experiments, we also devised the hyperbolic encoders to fuse drug and target similarity information into FLONE, to make it capable to handle triples corresponding to previously unseen drugs and targets for more challenging prediction scenarios. Availability and implementationSource code and dataset information are at: https://github.com/arantir123/DDT_triple_prediction. Contacts.he@cs.bham.ac.uk

bioinformatics↗

Nanoscaled discovery of a shunt rifamycin from Salinispora arenicola using a three-colour GFP-tagged Staphylococcus aureus macrophage infection assay.

Antimicrobial resistance has emerged as an urgent global public health threat, and development of novel therapeutics for treating infections caused by multi-drug resistant bacteria is urgent. Staphylococcus aureus is a major human and animal pathogen, responsible for high levels of morbidity and mortality worldwide. The intracellular survival of S. aureus in macrophages contributes to immune evasion, dissemination, and resilience to antibiotic treatment. Here, we present a confocal fluorescence imaging assay for monitoring macrophage infection by GFP-tagged Staphylococcus aureus as a front-line tool to identify antibiotic leads. The assay was employed in combination with nanoscaled chemical analyses to facilitate the discovery of a novel, active rifamycin analogue. Our findings indicate a promising new approach to the identification of anti-microbial compounds with macrophage intracellular activity. The novel antibiotic identified here may represent a useful addition to our armoury in tackling the silent pandemic of antimicrobial resistance.

cell biology↗

Detection and quantification of the heterogeneity of S. aureus bacterial populations to identify antibiotic-induced persistence

ObjectivesPersister cells are characterised as being viable but non-culturable, a state that preserves their metabolic energy to survive the environmental stress, which allows for recurrent infections. Detection of persisters is, therefore, not possible with standard culture-dependent methods. Furthermore, the effect of antibiotics on the induction of persisters has not been assessed. This study aimed to identify antibiotic-induced persistence and determine the percentage of heterogeneity.\n\nMethodsVancomycin, daptomycin and dalbavancin were assessed by standard MIC methods against selected Staphylococcus aureus strains. Replicates of MIC assays were stained with propidium iodide to quantify live/dead and a reactive oxygen species (ROS) dye to detect and quantify persisters using culture-independent single-cell sorting, independently. A comparative analysis was then performed.\n\nResultsDalbavancin showed the lowest MIC values against tested S. aureus strains followed by daptomycin and vancomycin. Cell sorting of vancomycin-, daptomycin- and dalbavancin-treated S. aureus strains showed a range of 1.9-10.2%, 17.7-62.9% and 7.5-77.6% live cells based on the strain, respectively, in which daptomycin, in particular, was a strong inducer of a persister population. Persisters represented 3.7-16% of the bacterial population.\n\nConclusionsThe culture-independent identification of antibiotic-induced persistence through studying at the single-cell level showed different efficacy of antibiotics than standard MIC. Vancomycin was the most effective antibiotic against tested strains followed by dalbavancin then daptomycin as assessed by cell sorting. Therefore, re-evaluation of standard MIC methods may be required to assess the efficacy of antibiotics. Additionally, the detection of daptomycin-associated persisters may provide an elucidation to the reported rapid resistance development in vivo.

microbiology↗