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BioAssay: AID 485363

Probe Development Summary for Inhibitors of Schistosoma Mansoni Peroxiredoxins

The following assay summarizes ongoing efforts in the development of chemical probes that inhibit Schistosoma Mansoni Peroxiredoxins. ..more
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AID: 485363
Data Source: NCGC (TGR1000)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-10-06
Modify Date: 2012-08-17
Target
Depositor Specified Assays
AIDNameTypeComment
485364qHTS Assay for the Inhibitors of Schistosoma Mansoni PeroxiredoxinsconfirmatoryqHTS
448Schistosoma Mansoni Peroxiredoxins (Prx2)confirmatorySchistosoma Mansoni Peroxiredoxins (Prx2) and thioredoxin glutathione reductase (TGR) coupled assay
1011Confirmation Concentration-Response Assay for Inhibitors of the Schistosoma mansoni Redox CascadeconfirmatoryConfirmation Concentration-Response Assay for Inhibitors of the Schistosoma mansoni Redox Cascade
Description:
The following assay summarizes ongoing efforts in the development of chemical probes that inhibit Schistosoma Mansoni Peroxiredoxins.

Schistosomiasis is a major neglected tropical disease that currently affects over 200 million. It is caused by different species of flatworms, such as Schistosoma mansoni. Over the last century, drugs to treat the disease have evolved from potassium antimonyl tartrate, artemisinin, oxamniquine, to praziquantel, with praziquantel remaining the universally-used single drug of choice over the past three decades. However, transmission rates have changed little with praziquantel, and there is evidence for the development of drug resistant parasites. Because there is currently no suitable alternative therapy available, there is an urgent need to identify new targets and drugs for schistosomiasis treatment. Thioredoxin glutathione reductase (TGR), one uniquely positioned S. mansoni enzyme, has been identified as a major component of the worms' distinct and compressed antioxidant "firewall". TGR is a multifunctional enzyme that catalyzes the interconversion between reduced and oxidized forms of both glutathione (GSH) and thioredoxins, thus making it an attractive new antiparasitic target.

This assay will be updated during the course of the probe development process.
Protocol
Please see related BioAssays for all protocols relevant to this probe development project: 448, 1011
Comment
Compound ranking comments will be added here as small molecule probes are developed and are annotated with bioassays in PubChem.
Additional Information
Grant Number: MH076449-01

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