Results 81 to 90 of about 1,018 (177)
Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB [PDF]
Journal of Medicinal Chemistry, 2009 Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas' disease and African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases for survival: cruzain for T. cruzi and TbCatB/rhodesain for T. brucei. A recent quantitative high-throughput screen of cruzain identified triazine nitriles, which are known ...
Bryan T, Mott +15 more
openaire +2 more sources
Structural representation of cruzain-ligand interfaces.
, 2019 3D and 2D interfaces of (A) cruzain-compound 1 and (B) cruzain-compound 2. In each diagram, the residues considered energetically relevant are labeled together with the name of atoms forming the main inter-molecular hydrogen bonds (red dashed lines in ...
Lilian Hernández Alvarez (739728) +3 more
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, 2023 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.
Renata Barbosa de Oliveira (14650037) +3 more
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Identification of a New Class of Nonpeptidic Inhibitors of Cruzain
, 2016 Cruzain is the major cysteine protease of Trypanosoma cruzi, which is the causative agent of Chagas disease and is a promising target for the development of new chemotherapy.
Katrien Brak (2300659) +3 more
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Kinetic Studies of Thiosemicarbazone Inhibitors of Cruzain, a Validated Target of Cruzain
, 2013 Chagas’ disease is caused by the flagellate protozoan Trypanosoma cruzi. As determined by the World Health Organization, effective therapeutic medications are needed for the treatment of Chagas’ disease.
Guillory, Joseph
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Comparison of betweenness centrality of each cruzain residue obtained from PENs.
, 2019 Representation of per-residue centrality calculated in each simulated system, i. e., (A) cruzain apo form, (B) cruzain-compound 1, (C) cruzain-compound 2, (D) cruzain-peptide, (E) cruzain-peptide-compound 1 and (F) cruzain-peptide-compound 2.
Lilian Hernández Alvarez (739728) +3 more
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Analysis of motions of the apo and holo forms of cruzain.
, 2019 Graphic representation of matrices corresponding to CP differences (ΔCP). The CP values corresponding to (A) cruzain-peptide, (B) cruzain-compound 1 and (C) cruzain-compound 2 were subtracted from those of the apo form, and the CP values of (D) cruzain ...
Lilian Hernández Alvarez (739728) +3 more
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Thirty Years in the Design and Development of Cruzain Inhibitors
Journal of the Brazilian Chemical SocietyCruzipain 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 enzyme) in 1995, this target has attracted the interest of many research groups for screening studies, structure-based and ligand ...
Gabriel Jasinski +2 more
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, 2020 Left. K777 in the active site of cruzain (PDB-ID: 1F2B). Right 33L in the active site of cruzain (PDB-ID 4QH6).
Fabiana Rosini (769679) +14 more
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Colocalization of cruzain and NF-κB P65.
, 2013 A–C. Representative examples of colocalization of labeled cruzain (A) (red fluorescence) and NF-κB P65 (B) (green fluorescence) in the flagellar pocket region and/or cell surface of interiorized transforming parasites (C, merge). D.
Ivy Hsieh (174545) +5 more
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