Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway.
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.
Gao
Jinbo
J
Department of Biology and Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Kowloon, Hong Kong, PR China.
Chu
Xiusheng
X
Qiu
Yongge
Y
Wu
Long
L
Qiao
Yuqin
Y
Wu
Jiasheng
J
Li
Ding
D
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
D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D008798:Mevalonic Acid