title: Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway.
abstract: The mevalonate pathway is an important drug target for the treatment of cancer and cardiovascular disease. We synthesized and studied a new type of nitrogen-containing bisphosphonate analogs and developed a sensitive end point assay method for enzyme FPPS, which was used for inhibitor screening. One potent FPPS inhibitor was discovered, and the structure-activity relationship of bisphosphonates for the enzyme inactivation was studied.
authors.affiliation: Department of Biology and Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Kowloon, Hong Kong, PR China.
authors.forename: Jinbo
authors.initials: J
authors.lastname: Gao
authors.forename: Xiusheng
authors.initials: X
authors.lastname: Chu
authors.forename: Yongge
authors.initials: Y
authors.lastname: Qiu
authors.forename: Long
authors.initials: L
authors.lastname: Wu
authors.forename: Yuqin
authors.initials: Y
authors.lastname: Qiao
authors.forename: Jiasheng
authors.initials: J
authors.lastname: Wu
authors.forename: Ding
authors.initials: D
authors.lastname: Li
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D055162:Biocatalysis; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008798:Mevalonic Acid / Q000378:metabolism*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D008798:Mevalonic Acid