A5008104047- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Education and Digital Technologies
- Synthesis and Biological Evaluation
- Education Pedagogy and Practices
- Click Chemistry and Applications
- Environmental Sustainability and Education
- Science and Education Research
- Geography and Environmental Studies
- Urban Development and Societal Issues
- Business and Management Studies
- Computational Drug Discovery Methods
- HIV/AIDS drug development and treatment
- Helminth infection and control
- Insect symbiosis and bacterial influences
- Plant biochemistry and biosynthesis
- Soil Management and Crop Yield
- Geography and Education Methods
- Melanoma and MAPK Pathways
- PI3K/AKT/mTOR signaling in cancer
- Biochemical and Molecular Research
- Peptidase Inhibition and Analysis
- Adenosine and Purinergic Signaling
- Parasites and Host Interactions
- Bioactive Compounds and Antitumor Agents
Universidade Federal de Minas Gerais
2011-2025
Grand Valley State University
2024-2025
Chagas disease remains a neglected tropical with limited therapeutic options and pressing need for new antichagasic agents. In this context, Cruzipain (CZP), the main cysteine protease of T. cruzi, has been validated as promising target reversible targeted covalent inhibitors (TCIs). Building upon our previous research, study reports phenyl thiosulfonate (TSO)-based TCIs, designed to optimize enzymatic performance enhance bioactivity translation from in vitro CZP inhibition cruzi-infected...
Abstract Cruzipains are the main papain-like cysteine proteases of Trypanosoma cruzi , protozoan parasite that causes Chagas disease. Encoded by a multigenic family, previous studies have estimated presence dozens copies spread over multiple chromosomes in different strains. Here, we describe complete gene repertoire cruzipain three strains, their genomic organization, and expression pattern throughout life cycle. Furthermore, analyzed primary sequence variations among distinct family...
We examined strains of Trypanosoma cruzi isolated from patients with acute Chagas disease that had been acquired by oral transmission in the state Santa Catarina, Brazil (2005) and two isolates obtained a marsupial (Didelphis aurita) vector (Triatoma tibiamaculata). These were characterised through their biological behaviour isoenzymic profiles genotyped according to new Taxonomy Consensus (2009) based on discrete typing unities, is, T. genotypes I-VI. All exhibited biodeme type II. In six...
Cruzipain (CZP), the major cysteine protease present in
The Serine/arginine-rich protein kinases (SRPK) are involved in pre-mRNA splicing control through the phosphorylation of SR family factors. Over last years, several studies have shown relevance SRPK for human cancers and their potential as promising drug targets. In this context, we previously selected three trifluoromethyl arylamides (named here SRVIC24, SRVIC30 SRVIC36) with improved vitro antileukemia effect ability impairing cellular activity SRPK. Given increasing amount reports on...
Cruzipain (CZP) is an essential cysteine protease of Trypanosoma cruzi, the etiological agent Chagas disease, and a promising druggable target. To date, no CZP inhibitors have reached clinical use, with research efforts mostly hampered by insufficient potency, limited target selectivity or lack bioactivity translation from isolated enzyme to parasite in cellular environments. In this study, we report design SH-1, 1,2,3-triazole-based targeted covalent inhibitor nanomolar potency (IC50 = 28...
Abstract Cruzipains are the main papain-like cysteine proteases of Trypanosoma cruzi , protozoan parasite that causes Chagas disease. Encoded by a multigenic family, previous studies have estimated presence dozens copies spread over multiple chromosomes in different strains. Here, we describe complete gene repertoire cruzipain three strains, their genomic organization, and expression pattern throughout life cycle. Furthermore, analyzed primary sequence variations among distinct family...
The cysteine protease cruzain is a Chagas disease target, exploited in computational studies. However, there no consensus on the protonation states of active site residues Cys25, His162, and Glu208 at enzyme's pH range. We evaluated impact different these docking calculations. Through retrospective study with inhibitors decoys, we compared performance virtual screening using four grids, varying Glu208. Based enrichment factors ROC plots, grids affected compound ranking overall charge...