Search Results - "Eck, Tyler"
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A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs
Published in PLoS neglected tropical diseases (01-03-2022)“…Filariasis, caused by a family of parasitic nematodes, affects millions of individuals throughout the tropics and is a major cause of acute and chronic…”
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2
Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate
Published in PLoS neglected tropical diseases (01-04-2023)“…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…”
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Expression, purification, and inhibition profile of dihydrofolate reductase from the filarial nematode Wuchereria bancrofti
Published in PloS one (22-05-2018)“…Filariasis is a tropical disease caused by the parasitic nematodes Wuchereria bancrofti and Brugia malayi. Known inhibitors of dihydrofolate reductase (DHFR)…”
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4
Effect of Non‐Active Site Amino Acid Residues on Inhibitor Selectivity
Published in The FASEB journal (01-04-2018)“…Enzyme inhibitors are important in biological processes and as pharmaceutical drugs, the cornerstone of modern medicine. It is necessary to build a…”
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5
A novel series of putative Brugia malayi histone demethylase inhibitors as potential anti-filarial drugs
Published in PLoS neglected tropical diseases (01-03-2022)“…Filariasis, caused by a family of parasitic nematodes, affects millions of individuals throughout the tropics and is a major cause of acute and chronic…”
Get full text
Journal Article -
6
Structure–Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials
Published in Journal of medicinal chemistry (14-03-2024)“…Controlling malaria requires new drugs against Plasmodium falciparum. The P. falciparum cGMP-dependent protein kinase (PfPKG) is a validated target whose…”
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Correction to “Structure–Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials”
Published in Journal of medicinal chemistry (25-07-2024)Get full text
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8
Characterization of Competitive Inhibitors of P. falciparum cGMP-Dependent Protein Kinase
Published in Chembiochem : a European journal of chemical biology (23-02-2022)“…P. falciparum cGMP-dependent protein kinase (PfPKG) is an enticing anti-malarial drug target. Novel chemotypes are needed because existing inhibitors have…”
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Mutational analysis confirms the presence of distal inhibitor-selectivity determining residues in B. stearothermophilus dihydrofolate reductase
Published in Archives of biochemistry and biophysics (15-10-2020)“…Many antibacterial and antiparasitic drugs work by competitively inhibiting dihydrofolate reductase (DHFR), a vital enzyme in folate metabolism. The…”
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10
Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP‐Dependent Protein Kinase
Published in Chembiochem : a European journal of chemical biology (05-04-2022)“…Plasmodium falciparum cGMP‐dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors…”
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11
Discovery of Imidazole-Based Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase
Published in ACS medicinal chemistry letters (09-12-2021)“…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…”
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Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase
Published in RSC medicinal chemistry (01-01-2020)“…The cGMP-dependent protein kinase in (PfPKG) plays multiple roles in the life cycle of the parasite. As a result, this enzyme is a potential target for new…”
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Discovery of isoxazolyl-based inhibitors of cGMP-dependent protein kinase
Published in RSC medicinal chemistry (29-01-2020)“…The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite. As a result, this enzyme is a…”
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