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The Ivermectin Related Compound Moxidectin Can Target Apicomplexan Importin α and Limit Growth of Malarial Parasites.
Cells
January 2025
Nuclear Signaling Laboratory, Monash Biomedicine Discovery Institute, Department of Biochemistry and Molecular Biology, Monash University, Clayton, VIC 3800, Australia.
Signal-dependent transport into and out of the nucleus mediated by members of the importin (IMP) superfamily is crucial for eukaryotic function, with inhibitors targeting IMPα being of key interest as anti-infectious agents, including against the apicomplexan species and , causative agents of malaria and toxoplasmosis, respectively. We recently showed that the FDA-approved macrocyclic lactone ivermectin, as well as several other different small molecule inhibitors, can specifically bind to and inhibit and IMPα functions, as well as limit parasite growth. Here we focus on the FDA-approved antiparasitic moxidectin, a structural analogue of ivermectin, for its IMPα-targeting and anti-apicomplexan properties for the first time.
View Article and Find Full Text PDFSynthesis strategies and anti-parasitic evaluation of novel compounds for chagas disease: Advancing drug discovery through structure-activity relationships.
Eur J Med Chem
December 2024
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, India. Electronic address:
This study presents a comprehensive exploration of the synthesis of novel compounds targeting Chagas Disease (CD) caused by Trypanosoma cruzi. It is a global health threat with over 6-7 million infections worldwide. Addressing challenges in current treatments, the investigation explores diverse compound classes, including thiazoles, thiazolidinone, imidazole, pyrazole, 1,6-diphenyl-1H-pyrazolo[3,4-b] pyridine, pyrrole, naphthoquinone, neolignan, benzeneacyl hydrazones, and chalcones-based compounds.
View Article and Find Full Text PDFDrug-induced retinal vein occlusion: a disproportionality analysis from the FDA adverse event reporting system (2004-2023).
Front Pharmacol
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Department of Ophthalmology, Hui'an County Hospital, Quanzhou, Fujian, China.
Introduction: Retinal vein occlusion (RVO) often causes irreversible visual impairment, making early prevention crucial. This study aims to identify associations between different medications and RVO and provide information for clinical practice.
Method: This study included reports of RVO from the FDA Adverse Event Reporting System (FAERS) database from the first quarter (Q1) of 2004 to the fourth quarter (Q4) of 2023.
Cannabinoids as cytotoxic agents and potential modulators of the human parasite Trichomonas vaginalis.
Biomed Pharmacother
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Structural Biology Laboratory, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil; Programa de Pós-graduação em Biologia Celular e Molecular, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil. Electronic address:
Trichomoniasis, a globally prevalent sexually transmitted infection caused by Trichomonas vaginalis, affects approximately 278 million people each year. It presents a challenge due to resistance to the current treatment, Metronidazole (MTZ), which is also associated with side effects. Cannabis sativa, with more than 100 phytocannabinoids and numerous studies for therapeutic applications, including parasitic infections, has undergone a significant shift in acceptance worldwide, highlighted by legalizations and substantial revenue projections.
View Article and Find Full Text PDFCase report: C57BL/6NTac and C57BL/6NCrl mice displaying neurological signs after deworming with ivermectin.
Lab Anim
December 2024
Department of Microbiology, Tumor and Cell Biology, Karolinska Institute, Stockholm, Sweden.
For over 40 years, ivermectin has served as an effective anti-parasitic drug used in human and veterinary medicine. In laboratory animal facilities it is used prophylactically or therapeutically to maintain the health status of the colony or experimentally in studies. Although ivermectin is generally safe to use, there are reports of neurotoxicity associated with ivermectin crossing the blood-brain barrier due to overdosing or blood-brain barrier dysfunction.
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