ArticleInternational journal for parasitology. Drugs and drug resistance2014
Target-based vs. phenotypic screenings in Leishmania drug discovery: A marriage of convenience or a dialogue of the deaf?
Article in International journal for parasitology. Drugs and drug resistance, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- Discovery of Potential Antileishmanial Compounds Through Phenotypic Screening of an Alkaloid Library.Molecules (Basel, Switzerland) · 2025Article
- Enhancing Antileishmanial Activity of Amidoxime-Based Compounds Bearing a 4,5-Dihydrofuran Scaffold: In Vitro Screening AgainstMolecules (Basel, Switzerland) · 2024Article
- Targeting Trypanothione Metabolism in Trypanosomatids.Molecules (Basel, Switzerland) · 2024Review
- Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years.Microorganisms · 2023Review
- Miltefosine and Nifuratel Combination: A Promising Therapy for the Treatment ofInternational journal of molecular sciences · 2023Article
- Three Alkaloids from an Apocynaceae Species,Plants (Basel, Switzerland) · 2020Article
- Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria.Marine drugs · 2020Review
- Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB.International journal for parasitology. Drugs and drug resistance · 2019Article
- A chronic bioluminescent model of experimental visceral leishmaniasis for accelerating drug discovery.PLoS neglected tropical diseases · 2019Article
- Antileishmanial Evaluation of the Leaf Latex ofEvidence-based complementary and alternative medicine : eCAM · 2019Article
- Challenges in drug discovery targeting TriTryp diseases with an emphasis on leishmaniasis.International journal for parasitology. Drugs and drug resistance · 2018Review
- Innovation in neglected tropical disease drug discovery and development.Infectious diseases of poverty · 2018Review
- Chemoinformatics Strategies for Leishmaniasis Drug Discovery.Frontiers in pharmacology · 2018Review
- Antileishmanial activity and tubulin polymerization inhibition of podophyllotoxin derivatives on Leishmania infantum.International journal for parasitology. Drugs and drug resistance · 2017Article
- Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani.ACS infectious diseases · 2017Article
- Unravelling the rate of action of hits in the Leishmania donovani box using standard drugs amphotericin B and miltefosine.PLoS neglected tropical diseases · 2017Article
- Experimental infection of Phlebotomus perniciosus by bioluminescent Leishmania infantum using murine model and artificial feeder.Memorias do Instituto Oswaldo Cruz · 2016Article
- A Replicative In Vitro Assay for Drug Discovery against Leishmania donovani.Antimicrobial agents and chemotherapy · 2016Article
- Next-generation antimicrobials: from chemical biology to first-in-class drugs.Archives of pharmacal research · 2015Review
- Infrared fluorescent imaging as a potent tool for in vitro, ex vivo and in vivo models of visceral leishmaniasis.PLoS neglected tropical diseases · 2015Article
Corrections and comments
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drug discovery programs sponsored by public or private initiatives pursue the same ambitious goal: a crushing defeat of major Neglected Tropical Diseases (NTDs) during this decade. Both target-based and target-free screenings have pros and cons when it comes to finding potential small-molecule leads among chemical libraries consisting of myriads of compounds. Within the target-based strategy, crystals of pathogen recombinant-proteins are being used to obtain three-dimensional (3D) structures in silico for the discovery of structure-based inhibitors. On the other hand, genetically modified parasites expressing easily detectable reporters are in the pipeline of target-free (phenotypic) screenings. Furthermore, lead compounds can be scaled up to in vivo preclinical trials using rodent models of infection monitoring parasite loads by means of cutting-edge bioimaging devices. As such, those preferred are fluorescent and bioluminescent readouts due to their reproducibility and rapidity, which reduces the number of animals used in the trials and allows for an earlier stage detection of the infective process as compared with classical methods. In this review, we focus on the current differences between target-based and phenotypic screenings in Leishmania, as an approach that leads to the discovery of new potential drugs against leishmaniasis.
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