Topic 166

schistosomiasis mansoni schistosoma drugs drug compounds worms parasite anti parasites neglected schistosome inhibitor compound people schistosomes treatment praziquantel tropical efficacy screening worm countries inhibits million targets inhibitors microbiology parasitic action schistosomula salvage including treated vaccine therapeutics inhibition caused development anthelmintic potent haematobium adult egg selective mass disease host homologues dhodh activity agents could new schistosomals evaluation toxicity identification other resistant flatworm agent pharmacological discovery activities target mg death lifecycle multidrug demonstrated interventions poorest ec50 inhibited overexpression antibiotic profiling tested liver active circulation uridine molecule infection trials induced into methanolic against highly 68 methodology pyrimidine novel concentrations selectivity lactone pzq venom

34 items. Top items listed below.

Schistosomes alter expression of immunomodulatory gene products following in vivo praziquantel exposure 166 64 10 3

Quorum sensing N-Acyl homoserine lactones are a new class of anti-schistosomal. 166 52 12 10

Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) is a druggable target involved in parasite survival, oviposition and stem cell proliferation. 166 12 3

Large-scale RNAi screening uncovers new therapeutic targets in the human parasite Schistosoma mansoni 166 3

A single-cell RNAseq atlas of the pathogenic stage of Schistosoma mansoni identifies a key regulator of blood feeding 166 57

Identifying and validating the presence of Guanine-Quadruplexes (G4) within the blood fluke parasite Schistosoma mansoni. 166

Vaccination with Schistosoma mansoni cholinesterases reduces parasite burden and egg viability in a mouse model of schistosomiasis 166 10

Capsaicin inhibits arginine kinase and exerts anti-Trypanosoma cruzi activity 166 44 10

Bioinformatics evaluation of the homologues of Schistosoma mansoni biomarker proteins of bladder cancer in other Schistosoma species 166

Ivermectin inhibits extracellular vesicle secretion from parasitic nematodes 166 10

Schistosoma haematobium extracellular vesicle proteins confer protection in a heterologous model of schistosomiasis 166 12 10

A multi-dimensional, time-lapse, high content screening platform applied to schistosomiasis drug discovery 166 18

Development of A Novel Highly Selective TLR8 Agonist for Cancer Immunotherapy 166 64 10 3

Morphological profiling of tubercule bacilli identifies drug pathways of action 166 79 12

The Synergism Between DHODH Inhibitors and Dipyridamole Leads to Metabolic Lethality in Acute Myeloid Leukemia 166 126 14 10 3

Identification and characterization of drug resistance mechanisms in cancer cells against Aurora kinase inhibitors CYC116 and ZM447439 166 126 14 10 9

JQ-1 ameliorates schistosomiasis liver fibrosis by suppressing JAK2 and STAT3 activation 10 3

Inhibition of the neuromuscular acetylcholine receptor with atracurium activates FOXO/DAF-16-induced longevity 166 90 3

A tale of two tails - efficient profiling of protein degraders by specific functional and target engagement readouts 166 45

Discovery of 5,5'-methylenedi-2,3-cresotic acid as a potent inhibitor of the HMGB1/CXCL12 heterocomplex using Virtual Screening and NMR validation 166 63 10

Enhancing the Antiviral Efficacy of RNA-Dependent RNA Polymerase Inhibition by Combination with Modulators of Pyrimidine Metabolism 166 41 10 3

PerSort facilitates characterization and elimination of persister subpopulation in mycobacteria 166 12 10

Schistosoma Japonicum infection in Treg-specific USP21 knock-out mice 27 10 3

Differential activity and expression of human 5β-reductase (AKR1D1) splice variants 166 10 3

Large CRISPR-Cas-induced deletions in the oxamniquine resistance locus of the human parasite Schistosoma mansoni 33 9

Antiviral Drug Screen of Kinase inhibitors Identifies Cellular Signaling Pathways Critical for SARS-CoV-2 Replication 44 1

Structure of Mpro from COVID-19 virus and discovery of its inhibitors 44 1

Role of selective Bioactive Compounds as an Angiotensin Converting Enzyme Inhibitor 166 115

The narrow-spectrum anthelmintic oxantel is a potent agonist of a novel acetylcholine receptor subtype in whipworms 64 10

Identification of an antiretroviral small molecule that appears to be a host-targeting inhibitor of HIV-1 assembly 41 12 10 3

Anti-oxidant and in-vitro α-amylase inhibitory activities of leaves and barks of Randia dumetorum 166 115

Dielectrophoresis assisted rapid, selective and single cell detection of antibiotic resistant bacteria with G-FETs 166 18 12

CRISPR/Cas9-mediated genome editing of Schistosoma mansoni acetylcholinesterase 33 10

A targeted computational screen of the SWEETLEAD database reveals FDA-approved compounds with anti-dengue viral activity 44 41 10

Inhibiting coronavirus replication in cultured cells by chemical ER stress 166 1

Antineoplastic kinase inhibitors: a new class of potent anti-amoebic compounds 44 10

Hydroxychloroquine-mediated inhibition of SARS-CoV-2 entry is attenuated by TMPRSS2 44 1

Massive-scale biological activity-based modeling identifies novel antiviral leads against SARS-CoV-2 44 1

Ebselen as a highly active inhibitor of PLProCoV2 44 1

Enisamium is a small molecule inhibitor of the influenza A virus and SARS-CoV-2 RNA polymerases 44 1

Coronavirus infection and PARP expression dysregulate the NAD Metabolome: an actionable component of innate immunity 166 41 3 1

Development of a fluorescence based, high-throughput SARS-CoV-2 3CLpro reporter assay 44 1

Hepatitis B virus Core protein nuclear interactome identifies SRSF10 as a host RNA-binding protein restricting HBV RNA production 41 3

A data-driven drug repositioning framework discovered a potential therapeutic agent targeting COVID-19 44 1

Characterisation of a Teladorsagia circumcincta glutathione transferase. 166 129 63 8

Discovery of clinically approved drugs capable of inhibiting SARS-CoV-2 in vitro infection using a phenotypic screening strategy and network-analysis to predict their potential to treat covid-19 44 1

In silico molecular target prediction unveils mebendazole as a potent MAPK14 inhibitor 7 3

Tumor Necrosis Factor and Schistosoma mansoni egg antigen Omega-1 shape distinct aspects of the early egg-induced granulomatous response 27 3

Therapeutic Drugs Targeting 2019-nCoV Main Protease by High-Throughput Screening 44 1

CETSA MS profiling for a comparative assessment of FDA approved antivirals repurposed for COVID-19 therapy identifies Trip13 as a Remdesivir off-target 44 41 1

The SARS-CoV-2 cytopathic effect is blocked with autophagy modulators 44 1

Structural determinants of persulfide-sensing specificity in a dithiol-based transcriptional regulator 166 63 8 3

Ambroxol Hydrochloride Inhibits the Interaction between Severe Acute Respiratory Syndrome Coronavirus 2 Spike Protein's Receptor Binding Domain and Recombinant Human ACE2. 36 1

Multidrug treatment with nelfinavir and cepharanthine against COVID-19 44 1

Serotonergic drugs inhibit CHIKV infection at different stages of the cell entry pathway 41 1

Identification of antiviral drug candidates against SARS-CoV-2 from FDA-approved drugs 44 1

TMPRSS2 and furin are both essential for proteolytic activation and spread of SARS-CoV-2 in human airway epithelial cells and provide promising drug targets 44 1

High-throughput cell-based assays for the preclinical development of DsbA inhibitors as antivirulence therapeutics. 52 12

Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease 44 1

Computational pharmacogenomics screen identifies synergistic statin-compound combinations as anti-breast cancer therapies 14 10 3

Evaluation of ExoU inhibitors in a Pseudomonas aeruginosa scratch infection assay 52 10

Identification of TMEM106B as proviral host factor for SARS-CoV-2 73 1

Potential microenvironment of SARS-CoV-2 infection in airway epithelial cells revealed by Human Protein Atlas database analysis 36 1

Inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 main protease by tafenoquine in vitro 44 1

Insight into vaccine development for Alpha-coronaviruses based on structural and immunological analyses of spike proteins 24 1

AMP-activated protein kinase: A key enzyme to manage nutritional stress responses in parasites with complex life cycles 102 3

ATR inhibition enhances 5-fluorouracil sensitivity independent of non-homologous end-joining and homologous recombination repair pathway 46 14 10 3

Role of RBC membrane protein palmitoylation in regulation of molecular topology and susceptibility to Plasmodium falciparum invasion 166 60 3

A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing 44 1

Histidine-Triad Hydrolases Provide Resistance to Peptide-Nucleotide Antibiotics 166 129 52 12 8 3

Inoculum effect of antimicrobial peptides 52 12

Discovery of COVID-19 Inhibitors Targeting the SARS-CoV2 Nsp13 Helicase 44 1

Identify potent SARS-CoV-2 main protease inhibitors via accelerated free energy perturbation-based virtual screening of existing drugs 44 1

Ionophore antibiotic X-206 is a potent and selective inhibitor of SARS-CoV-2 infection in vitro 44 1

The landscape of metabolic pathway dependencies in cancer cell lines 186 9 3

Bcr-Abl tyrosine kinase inhibitor imatinib as a potential drug for COVID-19 36 1

Characterisation of protease activity during SARS-CoV-2 infection identifies novel viral cleavage sites and cellular targets for drug repurposing 44 1

Bioinformatic analysis of shared B and T cell epitopes amongst relevant coronaviruses to human health: Is there cross-protection? 76 1

Non-invasive monitoring of drug action: a new live in vitro assay design for Chagas' disease drug discovery 10

Divide et Impera: Identification of Small-Molecule Inhibitors of HCMV Replication Interfering with Dimerization of DNA Polymerase Processivity Factor UL44 41 10 3

An artificial intelligence system reveals liquiritin inhibits SARS-CoV-2 by mimicking type I interferon 44 1

Morphological Cell Profiling of SARS-CoV-2 Infection Identifies Drug Repurposing Candidates for COVID-19 44 1

Antiviral treatment of SARS-CoV-2-infected hamsters reveals a weak effect of favipiravir and a complete lack of effect for hydroxychloroquine 44 1

Optimizing 3-dimensional human skin models to facilitate long-term development of Onchocerca volvulus, a debilitating obligatory human parasite 85 10

A Transferable Deep Learning Approach to Fast Screen Potent Antiviral Drugs against SARS-CoV-2 44 1

Drug repurposing screen identifies masitinib as a 3CLpro inhibitor that blocks replication of SARS-CoV-2 in vitro 44 1

PQS-Induced Outer Membrane Vesicles Enhance Biofilm Dispersion in Pseudomonas aeruginosa 52 12 10 3

Pre-clinical search of SARS-CoV-2 inhibitors and their combinations in approved drugs to tackle COVID-19 pandemic 44 1

Leish-ExP: a database of exclusive proteins from Leishmania parasite 121 12

Genoprotective effects of Chaga mushroom (Inonotus obliquus) polysaccharides in UVB-exposed embryonic zebrafish (Danio rerio) through coordinated expression of DNA repair genes 166 10 3

Dynamic metabolic reprogramming in dendritic cells: an early response to influenza infection that is essential for effector function 27 10 3

A dynamic regulatory interface on SARS-CoV-2 RNA polymerase 44 1

Prophylactic and Therapeutic Inhibition of In Vitro SARS-CoV-2 Replication by Oleandrin 44 1

Toxoplasmicidal in vitro effect of dehydroepiandrosterone on Toxoplasma gondii extracellular tachizoytes 10

AKT-like kinase promotes cell survival during nutritional stress in trypanosomatids 60 3

A Trypanosoma brucei ORFeome-based Gain-of-Function Library identifies genes that promote survival during melarsoprol treatment 33 9

Unravelling mechanisms of meropenem induced persistence facilitates identification of GRAS compounds with anti-persister activity against Acinetobacter baumannii 52 12 10

Host porphobilinogen deaminase deficiency confers malaria resistance in Plasmodium chabaudi but not in Plasmodium falciparum or Plasmodium berghei during intraerythrocytic growth 60 10 3

The folate antagonist methotrexate diminishes replication of the coronavirus SARS-CoV-2 and enhances the antiviral efficacy of remdesivir in cell culture models 44 1

System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion 60 10 3