Targeting thioredoxin glutathione reductase as a potential antischistosomal drug target.

Autor: Eweas AF; Department of Medicinal Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza, Egypt. Electronic address: eweas1@gmail.com., Allam G; Department of Microbiology, College of Medicine, Taif University, Taif, Saudi Arabia; Immunology Division, Department of Zoology, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt.
Jazyk: angličtina
Zdroj: Molecular and biochemical parasitology [Mol Biochem Parasitol] 2018 Oct; Vol. 225, pp. 94-102. Date of Electronic Publication: 2018 Oct 04.
DOI: 10.1016/j.molbiopara.2018.09.004
Abstrakt: Schistosomiasis represents a world health major problem affecting more than 206 million people worldwide. Up to date, praziquantel (PZQ) is the sole chemotherapeutic agent used in clinics for the treatment of schistosomiasis. The resistance to PZQ chemotherapy that has been emerged against some schistosome phenotypes represents the most serious PZQ-related problem so far. Therefore, it is clear that there is a substantial need to develop novel and effective antischistosomal agents in order to ensure the effective drug control of schistosomiasis in the future. It is well-documented that the thiol redox homeostasis of schistosomes is entirely based on a single enzyme named thioredoxin-glutathione reductase (TGR). Thus, TGR is an essential protein for the survival of schistosomes which means that TGR is a valid and promising target for the recent antischistosomal drug-discovery approaches. This review aimed to shed light on potential lead compounds that may inhibit TGR activity and consequently could be tested as a potential antischistsomal drugs. In the current review we discussed multiple drug discovery approaches for new compounds targeting TGR and its implementation.
(Copyright © 2018 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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