ReviewExpert opinion on drug discovery2013
Design or screening of drugs for the treatment of Chagas disease: what shows the most promise?
Review in Expert opinion on drug discovery, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- Triazole-Functionalized Jatrophone Derivatives as Antiprotozoal Agents AgainstPharmaceuticals (Basel, Switzerland) · 2026Article
- In vitro and in vivo studies on the activity and selectivity of butoconazole in experimental infection by Trypanosoma cruzi.Memorias do Instituto Oswaldo Cruz · 2025Article
- Exploring Benzo[h]chromene Derivatives as Agents against Protozoal and Mycobacterial Infections.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Identification of Aryl Polyamines Derivatives as Anti-Pharmaceutics · 2022Article
- Perspectives for a new drug candidate for Chagas disease therapy.Memorias do Instituto Oswaldo Cruz · 2022Article
- Relaxed Substrate Requirements of Sterol 14α-Demethylase fromJournal of medicinal chemistry · 2021Article
- Therapeutic Interventions for Countering Leishmaniasis and Chagas's Disease: From Traditional Sources to Nanotechnological Systems.Pathogens (Basel, Switzerland) · 2019Review
- CYP51 as drug targets for fungi and protozoan parasites: past, present and future.Parasitology · 2018Review
- Antitrypanosomal Activity of Sterol 14α-Demethylase (CYP51) Inhibitors VNI and VFV in the Swiss Mouse Models of Chagas Disease Induced by the Trypanosoma cruzi Y Strain.Antimicrobial agents and chemotherapy · 2017Article
- Antiprotozoal Activity of Triazole Derivatives of Dehydroabietic Acid and Oleanolic Acid.Molecules (Basel, Switzerland) · 2017Article
- Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 from Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2016Article
- Developments in the management of Chagas cardiomyopathy.Expert review of cardiovascular therapy · 2015Review
- VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.The Journal of infectious diseases · 2015Article
- Sequence variation in CYP51A from the Y strain of Trypanosoma cruzi alters its sensitivity to inhibition.FEBS letters · 2014Article
- Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14α-demethylase: two regions of the enzyme molecule potentiate its inhibition.Journal of medicinal chemistry · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
introductionEndemic in Latin America, Chagas disease is now becoming a serious global health problem, and yet has no financial viability for the pharmaceutical industry and remains incurable. In 2012, two antimycotic drugs inhibitors of fungal sterol 14α-demethylase (CYP51) - posaconazole and ravuconazole - entered clinical trials. Availability of the X-ray structure of the orthologous enzyme from the causative agent of the disease, protozoan parasite Trypanosoma cruzi, determined in complexes with posaconazole as well as with several experimental protozoa-specific CYP51 inhibitors opens an excellent opportunity to improve the situation. AREAS COVERED: This article summarizes the information available in PubMed and Google on the outcomes of treatment of the chronic Chagas disease. It also outlines the major features of the T. cruzi CYP51 structure and the possible structure-based strategies for rational design of novel T. cruzi specific drugs. EXPERT OPINION: There is no doubt that screenings for alternative drug-like molecules as well as mining the T. cruzi genome for novel drug targets are of great value and might eventually lead to groundbreaking discoveries. However, all newly identified molecules must proceed through the long, expensive and low-yielding drug optimization process, and all novel potential drug targets must be validated in terms of their essentiality and druggability. CYP51 is already a well-validated and highly successful target for clinical and agricultural antifungals. With minimal investments into the final stages of their development/trials, T. cruzi-specific CYP51 inhibitors can provide an immediate treatment for Chagas disease, either on their own or in combination with the currently available drugs.
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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.