ArticleMemorias do Instituto Oswaldo Cruz2009
Two approaches to discovering and developing new drugs for Chagas disease.
Article in Memorias do Instituto Oswaldo Cruz, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 66 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
66 citing papers in PubMed, 1 synthesis or guideline pooled it, 172 citations in OpenAlex.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Pyridyl-Imidazopyridine Derivatives Displaying Submicromolar Activity Against Trypanosoma cruzi.ChemMedChem · 2026Article
- Cruzain Inhibitors for Chagas Disease: Anticorrelated Optimisation Landscapes and the Multiparametric Path to Clinical Candidates.Chemical biology & drug design · 2026Review
- Thiosulfonate-Based Targeted Covalent Cruzipain Inhibitors with Enhanced Bioactivity Translation for Antichagasic Therapy.ACS medicinal chemistry letters · 2025Article
- Discovery of a Potent Triazole-Based Reversible Targeted Covalent Inhibitor of Cruzipain.ACS medicinal chemistry letters · 2025Article
- Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (Journal of medicinal chemistry · 2024Article
- Structure-Aided Computational Design of Triazole-Based Targeted Covalent Inhibitors of Cruzipain.Molecules (Basel, Switzerland) · 2024Article
- Extracellular Cysteine Proteases of Key Intestinal Protozoan Pathogens-Factors Linked to Virulence and Pathogenicity.International journal of molecular sciences · 2023Review
- Self-Masked Aldehyde Inhibitors of Human Cathepsin L Are Potent Anti-CoV-2 Agents.Frontiers in chemistry · 2022Article
- De Novo Design of Cathepsin B1 Inhibitors as Potential Anti-Schistosomal Agents Using Computational Studies.Advances and applications in bioinformatics and chemistry : AABC · 2022Article
- An Overview on Target-Based Drug Design against Kinetoplastid Protozoan Infections: Human African Trypanosomiasis, Chagas Disease and Leishmaniases.Molecules (Basel, Switzerland) · 2021Review
- Article
- Repurposing Carvedilol as a Novel Inhibitor of theFrontiers in cellular and infection microbiology · 2021Article
- Multiparameter Optimization of Trypanocidal Cruzain Inhibitors WithFrontiers in pharmacology · 2021Article
- Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.Journal of medicinal chemistry · 2020Article
- Benzimidazole inhibitors of the major cysteine protease ofFuture medicinal chemistry · 2019Article
- Successful Aspects of the Coadministration of Sterol 14α-Demethylase Inhibitor VFV and Benznidazole in Experimental Mouse Models of Chagas Disease Caused by the Drug-Resistant Strain of Trypanosoma cruzi.ACS infectious diseases · 2019Article
- Cell death pathways in pathogenic trypanosomatids: lessons of (over)kill.Cell death & disease · 2019Review
- Chagas Disease Treatment and Rational Drug Discovery: A Challenge That Remains.Frontiers in pharmacology · 2019Article
- Discovery of Non-Peptidic Compounds against Chagas Disease Applying Pharmacophore Guided Molecular Modelling Approaches.Molecules (Basel, Switzerland) · 2018Article
6 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
This review will focus on two general approaches carried out at the Sandler Center, University of California, San Francisco, to address the challenge of developing new drugs for the treatment of Chagas disease. The first approach is target-based drug discovery, and two specific targets, cytochrome P450 CYP51 and cruzain (aka cruzipain), are discussed. A 'proof of concept' molecule, the vinyl sulfone inhibitor K777, is now a clinical candidate. The preclinical assessment compliance for filing as an Investigational New Drug with the United States Food and Drug Administration (FDA) is presented, and an outline of potential clinical trials is given. The second approach to identifying new drug leads is parasite phenotypic screens in culture. The development of an assay allowing high throughput screening of Trypanosoma cruzi amastigotes in skeletal muscle cells is presented. This screen has the advantage of not requiring specific strains of parasites, so it could be used with field isolates, drug resistant strains or laboratory strains. It is optimized for robotic liquid handling and has been validated through a screen of a library of FDA-approved drugs identifying 65 hits.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.