Results 51 to 60 of about 1,018 (177)

Ligand-induced conformational selection predicts the selectivity of cysteine protease inhibitors.

open access: yesPLoS ONE, 2019
Cruzain, a cysteine protease of Trypanosoma cruzi, is a validated target for the treatment of Chagas disease. Due to its high similarity in three-dimensional structure with human cathepsins and their sequence identity above 70% in the active site regions,
Geraldo Rodrigues Sartori   +3 more
doaj   +1 more source

A validated and interpretable predictive model of cruzain inhibitors [PDF]

open access: yes, 2020
Abstract Chagas disease affects 8–11 million people worldwide, most of them living in Latin America. Moreover, migratory phenomenon have spread the infection beyond endemic areas. Efforts for the development of new pharmacological therapies are paramount, as the pharmacological profile of the two marketed drugs ...
Jose G. Rosas-Jimenez   +3 more
openaire   +1 more source

Structure-Based and Molecular Modeling Studies for the Discovery of Cyclic Imides as Reversible Cruzain Inhibitors With Potent Anti-Trypanosoma cruzi Activity

open access: yesFrontiers in Chemistry, 2019
Chagas disease causes ~10,000 deaths each year, mainly in Latin America, where it is endemic. The currently available chemotherapeutic agents are ineffective in the chronic stage of the disease, and the lack of pharmaceutical innovation for Chagas ...
Rafael A. A. Ferreira   +10 more
doaj   +1 more source

Cruzain Inhibitory Activity of the Leaf Essential Oil from an Undescribed Species of from Monteverde, Costa Rica

open access: yesNatural Product Communications, 2007
The leaf essential oil of Eugenia sp. nov. “San Bosco” inhibits cruzain, a cysteine protease from Trypanosoma cruzi, the parasitic protozoan responsible for Chagas disease, with an IC 50 of 36.4 μg/mL.
Sean L. Stokes   +4 more
doaj   +1 more source

Organometallic Gold(III) Complexes with Tridentate Halogen‐Substituted Thiosemicarbazones: Effects of Halogenation on Cytotoxicity and Anti‐Parasitic Activity

open access: yesEuropean Journal of Inorganic Chemistry, Volume 2019, Issue 41, Page 4455-4462, November 10, 2019., 2019
Halogenation of thiosemicarbazone ligands in cationic organometallic Au(III) complexes enhances their stability against hydrolysis and retains or enhances their activity against the parasite trypanosoma cruzi. Best results were obtained with a ligand, which contains two fluorine atoms in 3,5‐positions of an aromatic ring, [Au(dampH)(L‐3,5‐F)]Cl ...
Federico Salsi   +7 more
wiley   +1 more source

Residue centrality in cruzain analyzed systems.

open access: yes, 2019
For convenience, the centrality profiles are represented as a comparison between ligand-bound and reference systems, i. e., cruzain apo form (red lines) and cruzain-peptide complex (blue lines), and cruzain-ligand complexes (green lines): (A) cruzain ...
Lilian Hernández Alvarez (739728)   +3 more
core   +1 more source

Chemical Composition and Cruzain Inhibitory Activity of Bark Essential Oil from Monteverde, Costa Rica

open access: yesNatural Product Communications, 2007
American trypanosomiasis, Chagas disease, is a great cause of human morbidity and mortality in the Neotropics. Although there is currently no effective treatment for this parasitic disease, a number of potential biochemical targets have been identified ...
William N. Setzer   +6 more
doaj   +1 more source

Proteases as antimalarial targets: strategies for genetic, chemical, and therapeutic validation

open access: yesThe FEBS Journal, Volume 284, Issue 16, Page 2604-2628, August 2017., 2017
Proteases play a variety of biological functions in the malaria parasite. These include core biological processes such as protein homeostasis and traffic, but also parasite‐specific functions (haemoglobin degradation, parasite egress, red blood cell invasion).
Edgar Deu
wiley   +1 more source

Repositioning FDA Drugs as Potential Cruzain Inhibitors from Trypanosoma cruzi: Virtual Screening, In Vitro and In Vivo Studies

open access: yesMolecules, 2017
Chagas disease (CD) is a neglected disease caused by the parasite Trypanosoma cruzi, which affects underdeveloped countries. The current drugs of choice are nifurtimox and benznidazole, but both have severe adverse effects and less effectivity in chronic
Isidro Palos   +7 more
doaj   +1 more source

A Brief View of the Surface Membrane Proteins from Trypanosoma cruzi

open access: yesJournal of Parasitology Research, Volume 2017, Issue 1, 2017., 2017
Trypanosoma cruzi is the causal agent of Chagas’ disease which affects millions of people around the world mostly in Central and South America. T. cruzi expresses a wide variety of proteins on its surface membrane which has an important role in the biology of these parasites. Surface molecules of the parasites are the result of the environment to which
Ángel de la Cruz Pech-Canul   +3 more
wiley   +1 more source

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