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Opportunities and Challenges in Antiparasitic Drug Discovery

Opportunities and Challenges in Antiparasitic Drug Discovery

http://www.wikidata.org/entity/Q29999214

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Global phenotypic screening for antimalarials Mini review on tricyclic compounds as an inhibitor of trypanothione reductase Drug repurposing and human parasitic protozoan diseases Trypanocidal activity of marine natural products Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening The structure ofPlasmodium vivaxphosphatidylethanolamine-binding protein suggests a functional motif containing a left-handed helix One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening Evolutionary patterning: a novel approach to the identification of potential drug target sites in Plasmodium falciparum Advancing drug innovation for neglected diseases-criteria for lead progression Functional expression of parasite drug targets and their human orthologs in yeast Hit-to-lead development of the chamigrane endoperoxide merulin A for the treatment of African sleeping sickness Naphthoquinone derivatives exert their antitrypanosomal activity via a multi-target mechanism Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign CANDO and the infinite drug discovery frontier In vitro anti-Leishmania activity of tetracyclic iridoids from Morinda lucida, benth Repurposing the open access malaria box to discover potent inhibitors of Toxoplasma gondii and Entamoeba histolytica Anti-plasmodial activity of Dicoma tomentosa (Asteraceae) and identification of urospermal A-15-O-acetate as the main active compound A luciferase based viability assay for ATP detection in 384-well format for high throughput whole cell screening of Trypanosoma brucei brucei bloodstream form strain 427.Lessons learnt from assembling screening libraries for drug discovery for neglected diseases.In vitro anti-malarial activity of N6-modified purine analogs.Dragonamide E, a modified linear lipopeptide from Lyngbya majuscula with antileishmanial activity Anti-leishmanial activity of betulin derivatives.Repositioning of an existing drug for the neglected tropical disease Onchocerciasis.Discovery of novel benzoxaborole-based potent antitrypanosomal agents.New chemical scaffolds for human african trypanosomiasis lead discovery from a screen of tyrosine kinase inhibitor drugs Essential multimeric enzymes in kinetoplastid parasites: A host of potentially druggable protein-protein interactions.Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif.The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.Parasite-based screening and proteome profiling reveal orlistat, an FDA-approved drug, as a potential anti Trypanosoma brucei agent.Target assessment for antiparasitic drug discovery.Bioactivity guided fractionation of leaves extract of Nyctanthes arbor tristis (Harshringar) against P falciparum.Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.Target identification and validation for anthelmintic discovery.Malaria parasite carbonic anhydrase: inhibition of aromatic/heterocyclic sulfonamides and its therapeutic potential.Icacina senegalensis (Icacinaceae), traditionally used for the treatment of malaria, inhibits in vitro Plasmodium falciparum growth without host cell toxicity.Novel anti-plasmodial hits identified by virtual screening of the ZINC database.Niche metabolism in parasitic protozoa.Drug discovery for human African trypanosomiasis: identification of novel scaffolds by the newly developed HTS SYBR Green assay for Trypanosoma brucei.In vitro anti-plasmodial activity of Dicoma anomala subsp. gerrardii (Asteraceae): identification of its main active constituent, structure-activity relationship studies and gene expression profiling Plasmodium transmission blocking activities of Vernonia amygdalina extracts and isolated compounds.

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Opportunities and Challenges in Antiparasitic Drug Discovery

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Nature Reviews Drug Discovery

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Opportunities and Challenges in Antiparasitic Drug Discovery

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Alan Hudson

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Marie-Annick Mouriès

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Mary Bendig

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Richard Pink

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P2860

Identification of an antimalarial synthetic trioxolane drug development candidate

Traditional herbal medicines for malaria

Two interacting binding sites for quinacrine derivatives in the active site of trypanothione reductase: a template for drug design

Structure of 2C-methyl-D-erythritol 2,4- cyclodiphosphate synthase: an essential enzyme for isoprenoid biosynthesis and target for antimicrobial drug development.

Insights into antifolate resistance from malarial DHFR-TS structures

Mutations in dihydropteroate synthase are responsible for sulfone and sulfonamide resistance in Plasmodium falciparum

Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs

Hit and lead generation: beyond high-throughput screening

Drug development for neglected diseases: a deficient market and a public-health policy failure

Dual action of antimonial drugs on thiol redox metabolism in the human pathogen Leishmania donovani

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727-740

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3399433

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10.1038/NRD1824

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9

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