Beilstein Journal of Organic Chemistry, 2013 Inhibition of the Trypanosoma cruzi cysteine protease cruzain has been proposed as a therapeutic approach for the treatment of Chagas’ disease. Among the best-studied cruzain inhibitors to date is the vinylsulfone K777 (1), which has proven effective in ...
Jonathan W. Choy +17 more
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Immune complexes in chronic Chagas disease patients are formed by exovesicles from Trypanosoma cruzi carrying the conserved MASP N-terminal region [PDF]
, 2017 The exovesicles (EVs) are involved in pathologic host-parasite immune associations and have been recently used as biomarkers for diagnosis of infectious diseases.
De Pablos, Luis Miguel +5 more
core +3 more sources
A validated and interpretable predictive model of cruzain inhibitors [PDF]
, 2020 AbstractChagas 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 currently available, nifurtimox and ...
Jose G. Rosas-Jimenez +3 more
openaire +1 more source
Design and Synthesis of Cysteine Protease Inhibitors
Proceedings, 2017 We have been preparing new dipeptidyl inhibitors against parasitic cysteine proteases cruzain (related to Chagas disease) and rhodesain (related to Sleeping Sickness disease), and against human cathepsins. [...]
Florenci V. Gonzalez
doaj +1 more source
The effects of a plant proteinase inhibitor from Enterolobium contortisiliquum on human tumor cell lines [PDF]
, 2011 Supplementary to the efficient inhibition of trypsin, chymotrypsin, plasma kallikrein, and plasmin already described by the EcTI inhibitor from Enterolobium contortisiliquum, it also blocks human neutrophil elastase (K(iapp)=4.3 nM) and prevents phorbol ...
Bhoola K.D. +16 more
core +1 more source
Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain Inhibitors as anti-trypanosoma cruzi agents [PDF]
, 2020 The development of cruzain inhibitors has been driven by the urgent need to develop novel and more effective drugs for the treatment of Chagas' disease.
Andricopulo, A. D. +8 more
core +1 more source
Structure-based discovery of novel US28 small molecule ligands with different modes of action [PDF]
, 2017 The human cytomegalovirus-encoded G protein-coupled receptor US28 is a constitutively active receptor, which can recognize various chemokines. Despite the recent determination of its 2.9 Å crystal structure, potent and US28-specific tool compounds are ...
Abrahamian +41 more
core +2 more sources
Antibiotics, 2021 Metal-based drugs, including lanthanide complexes, have been extremely effective in clinical treatments against various diseases and have raised major interest in recent decades. Hence, in this work, a series of lanthanum (III) and cerium (III) complexes,
Alberto Aragón-Muriel +7 more
doaj +1 more source
Nitrofurazone and its nitroheterocyclic analogues: a study of the electrochemical behavior in aqueous medium [PDF]
, 2013 The biological action of drugs with potential antichagasic activities can be better understood by knowing their reduction mechanism. For this proposal, the electrochemical reduction of nitrofurazone (NF) and its analogues, nitrofurfurilidene ...
Brito, Charles de Lima +3 more
core +1 more source
approach to screen compounds active against parasitic nematodes of major socio-economic importance [PDF]
, 2011 Infections due to parasitic nematodes are common causes of morbidity and fatality around the world especially in developing nations. At present however, there are only three major classes of drugs for treating human nematode infections.
Varun Khanna, Shoba Ranganathan
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