ArticleInternational journal for parasitology. Drugs and drug resistance2012
Recent Developments in Sterol 14-demethylase Inhibitors for Chagas Disease.
Article in International journal for parasitology. Drugs and drug resistance, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 113 citations in OpenAlex.
- Albaconazole Polymeric Nanocapsules for TreatingPathogens (Basel, Switzerland) · 2025Article
- Machine Learning-Based Approach to Identify Inhibitors of Sterol-14-Alpha Demethylase: A Study on Chagas Disease.Bioinformatics and biology insights · 2024Article
- From Benznidazole to New Drugs: Nanotechnology Contribution in Chagas Disease.International journal of molecular sciences · 2023Review
- Navigating drug repurposing for Chagas disease: advances, challenges, and opportunities.Frontiers in pharmacology · 2023Review
- Small molecule mediated inhibition of protein cargo recognition by peroxisomal transport receptor PEX5 is toxic to Trypanosoma.Scientific reports · 2022Article
- Endogenous Sterol Synthesis Is Dispensable forFrontiers in microbiology · 2022Article
- Administration of artinm lectin reduces the severity of the acute phase infection withFASEB bioAdvances · 2021Article
- Immunomodulation for the Treatment of Chronic Chagas Disease Cardiomyopathy: A New Approach to an Old Enemy.Frontiers in cellular and infection microbiology · 2021Review
- Long term follow-up of Trypanosoma cruzi infection and Chagas disease manifestations in mice treated with benznidazole or posaconazole.PLoS neglected tropical diseases · 2020Article
- Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria.Marine drugs · 2020Review
- Structure, Properties, and Function of Glycosomes inFrontiers in cellular and infection microbiology · 2020Review
- A new chemotype with promise against Trypanosoma cruzi.Bioorganic & medicinal chemistry letters · 2020Article
- Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii.Bioorganic & medicinal chemistry · 2019Article
- Potent and selective inhibitors for M32 metallocarboxypeptidases identified from high-throughput screening of anti-kinetoplastid chemical boxes.PLoS neglected tropical diseases · 2019Article
- In vitro evaluation of arylsubstituted imidazoles derivatives as antiprotozoal agents and docking studies on sterol 14α-demethylase (CYP51) from Trypanosoma cruzi, Leishmania infantum, and Trypanosoma brucei.Parasitology research · 2019Article
- Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi.Bioorganic & medicinal chemistry · 2019Article
- CYP51 as drug targets for fungi and protozoan parasites: past, present and future.Parasitology · 2018Review
- Experimental and Clinical Treatment of Chagas Disease: A Review.The American journal of tropical medicine and hygiene · 2017Review
- Genome-wide mutagenesis and multi-drug resistance in American trypanosomes induced by the front-line drug benznidazole.Scientific reports · 2017Article
- Rapid Chagas Disease Drug Target Discovery Using Directed Evolution in Drug-Sensitive Yeast.ACS chemical biology · 2017Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 2 countries.
Funding
Abstract
The protozoan parasite, Trypanosoma cruzi, causes the most prevalent parasitic infection in the American continent. It gives rise to life-long infection in humans and results in severe cardiomyopathy or other life-threatening manifestations (Chagas disease) in ~30% of those infected. Animal models and clinical studies indicate that etiological treatment of the infection reduces the risk of developing the disease manifestations. Unfortunately, the existing chemotherapeutics have suboptimal antiparasitic activity and cause significant side effects in many patients, thus better anti-trypanosomal drugs are greatly needed. The sterol biosynthesis pathway has received attention as a target for the development of new drugs for Chagas disease. In particular, inhibitors of sterol 14-demethylase (CYP51) are shown to be extremely active on Trypanosoma cruzi in vitro and in animal models. Antifungal drugs (i.e. azoles) in clinical use or in clinical studies have been extensively tested preclinically on Trypanosoma cruzi with posaconazole and ravuconazole demonstrating the most promising activity. As a result, posaconazole and a pro-drug of ravuconazole (E1224) are currently being evaluated in Phase II studies for Chagas disease. Additional CYP51 inhibitors that are specifically optimized for anti-Trypanosoma cruzi activity are in development by academia. These represent an alternative to proprietary antifungal drugs if the latter fall short in clinical trials or are too expensive for widespread clinical use in disease endemic countries. The research over the next few years will help define the role of CYP51 inhibitors, alone or in combination with other drugs, for managing patients with Chagas disease.
Identifiers
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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.