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A Pyridyl-Furan Series Developed from the Open Global Health Library Block Red Blood Cell Invasion and Protein Trafficking in Plasmodium falciparum through Potential Inhibition of the Parasite's PI4KIIIB Enzyme.
Ling DB, Nguyen W, Looker O, Razook Z, McCann K, Barry AE, Scheurer C, Wittlin S, Famodimu MT, Delves MJ, Bullen HE, Crabb BS, Sleebs BE, Gilson PR. Ling DB, et al. ACS Infect Dis. 2023 Sep 8;9(9):1695-1710. doi: 10.1021/acsinfecdis.3c00138. Epub 2023 Aug 28. ACS Infect Dis. 2023. PMID: 37639221 Free PMC article.
Parasites selected for resistance to a related compound, MMV396797, were also resistant to WEHI-518 as well as KDU731, an inhibitor of the phosphatidylinositol kinase PfPI4KIIIB, suggesting that this kinase is the target of the pyridyl-furan series. ...
Parasites selected for resistance to a related compound, MMV396797, were also resistant to WEHI-518 as well as KDU731, an inhibitor o …
Novel treatment strategies and drugs in development for cryptosporidiosis.
Chavez MA, White AC Jr. Chavez MA, et al. Expert Rev Anti Infect Ther. 2018 Aug;16(8):655-661. doi: 10.1080/14787210.2018.1500457. Epub 2018 Jul 17. Expert Rev Anti Infect Ther. 2018. PMID: 30003818 Review.
Inhibition of Plasmodium lipid kinase PI(4)K8 of Cryptosporidium by KDU731 greatly reduced oocyst shedding and improved diarrhea in calves with limited effects on the human PI(4)K. ...
Inhibition of Plasmodium lipid kinase PI(4)K8 of Cryptosporidium by KDU731 greatly reduced oocyst shedding and improved diarrhea in c …
New Tools for Cryptosporidium Lead to New Hope for Cryptosporidiosis.
Ward HD. Ward HD. Trends Parasitol. 2017 Sep;33(9):662-664. doi: 10.1016/j.pt.2017.07.004. Epub 2017 Jul 24. Trends Parasitol. 2017. PMID: 28750950
The pyrazolopyridine KDU731 is a promising drug candidate for treatment of diarrhea caused by Cryptosporidium in young children in the resource-limited world. KDU731, a PI (4) kinase inhibitor, blocks Cryptosporidium infection in vitro and in vivo in immunocompromis …
The pyrazolopyridine KDU731 is a promising drug candidate for treatment of diarrhea caused by Cryptosporidium in young children in th …
A Cryptosporidium PI(4)K inhibitor is a drug candidate for cryptosporidiosis.
Manjunatha UH, Vinayak S, Zambriski JA, Chao AT, Sy T, Noble CG, Bonamy GMC, Kondreddi RR, Zou B, Gedeck P, Brooks CF, Herbert GT, Sateriale A, Tandel J, Noh S, Lakshminarayana SB, Lim SH, Goodman LB, Bodenreider C, Feng G, Zhang L, Blasco F, Wagner J, Leong FJ, Striepen B, Diagana TT. Manjunatha UH, et al. Nature. 2017 Jun 15;546(7658):376-380. doi: 10.1038/nature22337. Epub 2017 May 31. Nature. 2017. PMID: 28562588 Free PMC article.
Screening a library of compounds with anti-parasitic activity, we identify pyrazolopyridines as inhibitors of Cryptosporidium parvum and Cryptosporidium hominis. Oral treatment with the pyrazolopyridine KDU731 results in a potent reduction in intestinal infection of immuno …
Screening a library of compounds with anti-parasitic activity, we identify pyrazolopyridines as inhibitors of Cryptosporidium parvum and Cry …