Targeting a uniquely nonspecific prenyl synthase with bisphosphonates to combat cryptosporidiosis.
|Abstract||Cryptosporidiosis is a neglected disease without a wholly effective drug. We present a study demonstrating nitrogen-containing bisphosphonates (N-BPs) to be capable of inhibiting Cryptosporidium parvum at low micromolar concentrations in infected MDCK cells. Predictably, the mechanism of action is based on inhibition of biosynthesis of isoprenoids but the target enzyme is unexpectedly a distinctive C. parvum enzyme dubbed nonspecific polyprenyl p ... [truncated at 450 characters in length]|
|Author||Artz, Jennifer D; Dunford, James E; Arrowood, Michael J; et al|
|Subject||Animals Anti-Infective Agents Cattle Cells, Cultured Chromatography, Liquid Cryptosporidiosis Cryptosporidium parvum Crystallography, X-Ray Dimethylallyltranstransferase Diphosphonates Fluorescent Antibody Technique Humans Inhibitory Concentration 50 Models, Molecular Molecular Structure Protein Prenylation therapeutic use drug therapy drug effects enzymology antagonists and inhibitors metabolism pharmacology therapeutic use|