AI Article Synopsis
- Scientists found a way to target a specific enzyme, GSK-3, to fight a parasite that causes diseases.
- They tested compounds from their own collection and another collection to find new medicines that could stop this enzyme.
- The researchers discovered new types of chemicals that could help create effective treatments against the parasite in the future.
Article Abstract
Previous reports have validated the glycogen synthase kinase-3 (GSK-3) as a druggable target against the human protozoan parasite . This prompted us to search for new leishmanicidal scaffolds as inhibitors of this enzyme from our in-house library of human GSK-3β inhibitors, as well as from the Leishbox collection of leishmanicidal compounds developed by GlaxoSmithKline. As a result, new leishmanicidal inhibitors acting on GSK-3 at micromolar concentrations were found. These inhibitors belong to six different chemical classes (thiadiazolidindione, halomethylketone, maleimide, benzoimidazole, -phenylpyrimidine-2-amine and oxadiazole). In addition, the binding mode of the most active compounds into GSK-3 was approached using computational tools. On the whole, we have uncovered new chemical scaffolds with an appealing prospective in the development and use of GSK-3 inhibitors against this infectious protozoan.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6882465 | PMC |
| http://dx.doi.org/10.1080/14756366.2019.1693704 | DOI Listing |
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