Schistosoma mansoni cathepsin D1: Biochemical and biophysical characterization of the recombinant enzyme expressed in HEK293T cells

Araujo-Montoya, Bogar O.; Senger, Mário Roberto; Gomes, Bárbara Figueira; Harris, Gemma; Owens, Raymond J.; Silva, Floriano Paes

doi:10.1016/j.pep.2019.105532

Cited by 2 publications

(1 citation statement)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A homology modelling study and SAR analysis with peptidomimetic compounds designed against SjCD1 revealed unique structural features for achieving selectivity to this enzyme (144). Recombinant SmCD1 was recently expressed in HEK293 cells, characterized biophysically and biochemically (153). This is an important step towards further exploring this enzyme in TDD, since they can be considered promising druggable targets as demonstrated in the past with the development of HIV-1 protease inhibitors.…”

Section: Target-based Screeningmentioning

confidence: 99%

Schistosomiasis Drug Discovery in the Era of Automation and Artificial Intelligence

et al. 2021

View full text Add to dashboard Cite

Schistosomiasis is a parasitic disease caused by trematode worms of the genus Schistosoma and affects over 200 million people worldwide. The control and treatment of this neglected tropical disease is based on a single drug, praziquantel, which raises concerns about the development of drug resistance. This, and the lack of efficacy of praziquantel against juvenile worms, highlights the urgency for new antischistosomal therapies. In this review we focus on innovative approaches to the identification of antischistosomal drug candidates, including the use of automated assays, fragment-based screening, computer-aided and artificial intelligence-based computational methods. We highlight the current developments that may contribute to optimizing research outputs and lead to more effective drugs for this highly prevalent disease, in a more cost-effective drug discovery endeavor.

show abstract

Section: Target-based Screeningmentioning

confidence: 99%