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   Articles with "cruzain" as a keyword



Leveraging the cruzain S3 subsite to increase affinity for reversible covalent inhibitors.

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recommendations! Published in 2018 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2018.04.006

Abstract: Cruzain is the major cysteine protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Reversible covalent cruzain inhibitors can block the steps of cell differentiation in the parasite and kill the organism. To this… read more here.

Keywords: affinity; leveraging cruzain; cruzain; cruzain subsite ... See more keywords

Experimental and Computational Study of Aryl-thiosemicarbazones Inhibiting Cruzain Reveals Reversible Inhibition and a Stepwise Mechanism

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recommendations! Published in 2023 at "Journal of chemical information and modeling"

DOI: 10.1021/acs.jcim.2c01566

Abstract: Trypanosoma cruzi is a parasite that infects about 6-7 million people worldwide, mostly in Latin America, causing Chagas disease. Cruzain, the main cysteine protease of T. cruzi, is a validated target for developing drug candidates… read more here.

Keywords: experimental computational; compound; inhibition; cruzain ... See more keywords

Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach

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recommendations! Published in 2019 at "PLoS ONE"

DOI: 10.1371/journal.pone.0211227

Abstract: Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are… read more here.

Keywords: novel allosteric; allosteric inhibitors; site; allosteric mechanism ... See more keywords

Thirty Years in the Design and Development of Cruzain Inhibitors

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recommendations! Published in 2024 at "Journal of the Brazilian Chemical Society"

DOI: 10.21577/0103-5053.20240115

Abstract: Cruzipain is the principal protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Since its discovery in the 1980s and the resolution of the crystal structure of cruzain (a truncated recombinant form of the… read more here.

Keywords: design development; cruzain inhibitors; years design; cruzain ... See more keywords

Screening the Pathogen Box to Discover and Characterize New Cruzain and TbrCatL Inhibitors

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recommendations! Published in 2023 at "Pathogens"

DOI: 10.3390/pathogens12020251

Abstract: Chagas disease and Human African Trypanosomiasis, caused by Trypanosoma cruzi and T. brucei, respectively, pose relevant health challenges throughout the world, placing 65 to 70 million people at risk each. Given the limited efficacy and… read more here.

Keywords: cruzain; pathogen box; cruzain tbrcatl; screening pathogen ... See more keywords