Tyler Eck
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View article: An orally available PfPKG inhibitor blocks sporozoite infection of the liver
An orally available PfPKG inhibitor blocks sporozoite infection of the liver Open
Malaria remains a global health threat exacerbated by emerging resistance to antimalarial therapies and insecticides, climate-driven outbreaks, and limited chemoprotective options. Here, we report the characterization of RUPB-61 , the firs…
View article: Versatile Imidazole Scaffold with Potent Activity against Multiple Apicomplexan Parasites
Versatile Imidazole Scaffold with Potent Activity against Multiple Apicomplexan Parasites Open
Malaria, toxoplasmosis, and cryptosporidiosis are caused by apicomplexan parasites Plasmodium spp., Toxoplasma gondii, and Cryptosporidium parvum, respectively, and pose major health challenges. Their therapies are inadequate, ineffective …
View article: Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate
Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate Open
Lymphatic filariasis is a debilitating illness with an estimated 50 million cases as of 2018. The majority of cases are caused by the parasitic worm W . bancrofti and additional cases by the worms B . malayi and B . timori . Dihydrofolate …
View article: A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs
A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs Open
Filariasis, caused by a family of parasitic nematodes, affects millions of individuals throughout the tropics and is a major cause of acute and chronic morbidity. Current drugs are largely used in mass drug administration programs aimed at…
View article: A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs
A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs Open
Filariasis, caused by a family of parasitic nematodes, affects millions of individuals throughout the tropics and is a major cause of acute and chronic morbidity. Current drugs are largely used in mass drug administration programs aimed at…
View article: Characterization of Competitive Inhibitors of <i>Plasmodium falciparum</i> cGMP‐Dependent Protein Kinase**
Characterization of Competitive Inhibitors of <i>Plasmodium falciparum</i> cGMP‐Dependent Protein Kinase** Open
Plasmodium falciparum cGMP‐dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors have safety issues that may prevent further development. This work demonstrates is…
View article: Discovery of Imidazole-Based Inhibitors of <i>Plasmodium falciparum</i> cGMP-Dependent Protein Kinase
Discovery of Imidazole-Based Inhibitors of <i>Plasmodium falciparum</i> cGMP-Dependent Protein Kinase Open
The discovery of new targets for the treatment of malaria, in particular those aimed at the pre-erythrocytic stage in the life cycle, advanced with the demonstration that orally administered inhibitors of Plasmodium falciparum cGMP-depende…
View article: Discovery of imidazole-based inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase
Discovery of imidazole-based inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase Open
The discovery of new targets for treatment of malaria and in particular those aimed at the pre-erythrocytic stage in the life cycle, advanced with the demonstration that orally administered inhibitors of Plasmodium falciparum cGMP-dependen…
View article: Discovery of novel potent, cell-permeable inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase
Discovery of novel potent, cell-permeable inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase Open
The discovery of new targets for treatment of malaria advanced with the demonstration that orally administered inhibitors of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG) could clear infection in a murine model. This enthusia…
View article: Characterization of novel competitive inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase
Characterization of novel competitive inhibitors of <i>P. falciparum</i> cGMP-dependent protein kinase Open
P. falciparum cGMP-dependent protein kinase (PfPKG) is an enticing anti-malarial drug target. Structurally novel isoxazole-based compounds were shown to be ATP competitive inhibitors of PfPKG. Isoxazoles 3 and 5 had K i values of 0.7 ± 0.2…
View article: Discovery of isoxazolyl-based inhibitors of <i>Plasmodium falciparum</i> cGMP-dependent protein kinase
Discovery of isoxazolyl-based inhibitors of <i>Plasmodium falciparum</i> cGMP-dependent protein kinase Open
The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite.
View article: Expression, purification, and inhibition profile of dihydrofolate reductase from the filarial nematode Wuchereria bancrofti
Expression, purification, and inhibition profile of dihydrofolate reductase from the filarial nematode Wuchereria bancrofti Open
Filariasis is a tropical disease caused by the parasitic nematodes Wuchereria bancrofti and Brugia malayi. Known inhibitors of dihydrofolate reductase (DHFR) have been previously shown to kill Brugia malayi nematodes and to inhibit Brugia …