Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis

MJ Doenhoff, D Cioli, J Utzinger - Current opinion in infectious …, 2008 - journals.lww.com
Use of PZQ will increase in the foreseeable future, whether given alone or coadministered
with other anthelminthics in integrated control programmes. PZQ resistance remains a threat …

Glutathione and infection

D Morris, M Khurasany, T Nguyen, J Kim… - … et Biophysica Acta (BBA …, 2013 - Elsevier
BACKGROUND: The tripeptide γ-glutamylcysteinylglycine or glutathione (GSH) has
demonstrated protective abilities against the detrimental effects of oxidative stress within the …

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

A Jadhav, RS Ferreira, C Klumpp, BT Mott… - Journal of medicinal …, 2010 - ACS Publications
The perceived and actual burden of false positives in high-throughput screening has
received considerable attention; however, few studies exist on the contributions of distinct …

Inhibition of Schistosoma mansoni thioredoxin-glutathione reductase by auranofin: structural and kinetic aspects

F Angelucci, AA Sayed, DL Williams, G Boumis… - Journal of Biological …, 2009 - ASBMB
Schistosomiasis is a parasitic disease affecting over 200 million people currently treated
with one drug, praziquantel. A possible drug target is the seleno-protein thioredoxin …

Identification of oxadiazoles as new drug leads for the control of schistosomiasis

AA Sayed, A Simeonov, CJ Thomas, J Inglese… - Nature medicine, 2008 - nature.com
Abstract Treatment for schistosomiasis, which is responsible for more than 280,000 deaths
annually, depends almost exclusively on praziquantel. Millions of people are treated …

Thioredoxin reductase and its inhibitors

F Saccoccia, F Angelucci, G Boumis… - Current Protein and …, 2014 - benthamdirect.com
Thioredoxin plays a crucial role in a wide number of physiological processes, which span
from reduction of nucleotides to deoxyriboucleotides to the detoxification from xenobiotics …

Praziquantel: its use in control of schistosomiasis in sub-Saharan Africa and current research needs

MJ Doenhoff, P Hagan, D Cioli, V Southgate… - Parasitology, 2009 - cambridge.org
Treatment with praziquantel (PZQ) has become virtually the sole basis of schistosomiasis
control in sub-Saharan Africa and elsewhere, and the drug is reviewed here in the context of …

Antischistosomal agents: state of art and perspectives

EM Lago, RP Xavier, TR Teixeira, LM Silva… - Future Medicinal …, 2018 - Taylor & Francis
Praziquantel has remained the drug of choice for schistosomiasis chemotherapy for almost
40 years. The pressing need to develop a new antischistosomal drug may necessitate …

Tackling assay interference associated with small molecules

L Tan, S Hirte, V Palmacci, C Stork… - Nature Reviews …, 2024 - nature.com
Biochemical and cell-based assays are essential to discovering and optimizing efficacious
and safe drugs, agrochemicals and cosmetics. However, false assay readouts stemming …

A robotic platform for quantitative high-throughput screening

S Michael, D Auld, C Klumpp, A Jadhav… - Assay and drug …, 2008 - liebertpub.com
High-throughput screening (HTS) is increasingly being adopted in academic institutions,
where the decoupling of screening and drug development has led to unique challenges, as …