Results 141 to 150 of about 11,937 (188)

Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase

Bioorganic & Medicinal Chemistry Letters, 2010
A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhibitors into the isopentenyl pyrophosphate (IPP) and the geranyl pyrophosphate (GPP) substrate sub-pockets of the enzyme are presented.
Joris W, De Schutter, Serge, Zaretsky, Sarah, Welbourn, Arnim, Pause, Youla S, Tsantrizos   +4 more
openaire   +2 more sources

Farnesyl Pyrophosphate Synthase Is the Molecular Target of Nitrogen-Containing Bisphosphonates

Biochemical and Biophysical Research Communications, 1999
Bisphosphonates (Bps), inhibitors of osteoclastic bone resorption, are used in the treatment of skeletal disorders. Recent evidence indicated that farnesyl pyrophosphate (FPP) synthase and/or isopentenyl pyrophosphate (IPP) isomerase is the intracellular target(s) of bisphosphonate action. To examine which enzyme is specifically affected, we determined
Beek, E. van, Pieterman, E., Cohen, L., Löwik, C., Papapoulos, S.   +4 more
openaire   +3 more sources

Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway

Chemical Communications, 2010
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.
Jinbo, Gao, Xiusheng, Chu, Yongge, Qiu, Long, Wu, Yuqin, Qiao, Jiasheng, Wu, Ding, Li   +6 more
openaire   +2 more sources

Molecular characterization and expression analysis of two farnesyl pyrophosphate synthase genes involved in rubber biosynthesis in Hevea brasiliensis

Industrial Crops and Products, 2017
Rizhong Zeng
exaly   +2 more sources

Investigation of the Catalytic Mechanism of Farnesyl Pyrophosphate Synthase by Computer Simulation

The Journal of Physical Chemistry B, 2006
Farnesyl pyrophosphate synthase (FPPS) catalyses the formation of a key cellular intermediate in isoprenoid metabolic pathways, farnesyl pyrophosphate, by the sequential head-to-tail condensation of two molecules of isopentenyl diphosphate (IPP) with dimethylallyl diphosphate (DMAPP).
Verónica Muriel, Sanchez, Alejandro, Crespo, J Silvio, Gutkind, Adrián Gustavo, Turjanski   +3 more
openaire   +2 more sources

Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase

Biotechnology Letters, 2010
Farnesyl pyrophosphate synthase (FPPS) is an essential enzyme in the mevalonate pathway and might be relevant to hypertension and other cardiovascular diseases. FPPS transgenic mice were produced by microinjecting a construct with the FPPS gene into fertilized eggs derived from an inbred C57BL/6 strain.
Jian, Yang, Jun-Chang, Jiang, Lei, Guo, Shen-Jiang, Hu   +3 more
openaire   +2 more sources

Exploiting the Geranylgeranyl‐Pyrophosphate‐Sensing N‐Terminal Domain of HMG‐CoA Reductase 2 to Regulate Farnesyl Pyrophosphate Synthase (Erg20p) for Improved Monoterpene Production in Saccharomyces cerevisiae

Yeast
Dynamic downregulation of the endogenous farnesyl pyrophosphate (FPP) synthase (Erg20p) is crucial to engineer heterologous monoterpene production in the yeast Saccharomyces cerevisiae.
Zeyu Lu, Samuel Evans, Liam McDonnell, Nagasri Bandari, Yilun Weng, Wanli Jin, Robert E Speight, Gerhard Schenk, Christopher B. Howard, Claudia E Vickers, Bingyin Peng   +10 more
semanticscholar   +1 more source

Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase

Journal of Medicinal Chemistry, 2015
Farnesyl pyrophosphate synthase (FPPS) catalyzes the condensation of isopentenyl pyrophosphate (IPP) and dimethylallyl pyrophosphate to FPP and is known to be a molecular target of osteoporosis drugs, such as risedronate (RIS), which is a nitrogen-containing bisphosphonate.
Takeshi, Yokoyama, Mineyuki, Mizuguchi, Andreas, Ostermann, Katsuhiro, Kusaka, Nobuo, Niimura, Tabias E, Schrader, Ichiro, Tanaka   +6 more
openaire   +2 more sources

A Farnesyl Pyrophosphate Synthase Gene Is Expressed in Fat Body Regulates Cantharidin Synthesis in Male Epicauta impressicornis Blister Beetle.

Journal of Agricultural and Food Chemistry
Blister beetles of Epicauta impressicornis have attracted attention because they contain a large amount of cantharidin (CTD). To date, however, the synthesis and transfer of CTD in adults of E. impressicornis are largely unknown. Here, we showed that the
Zhicheng Zhou, Dingze Mang, G. Smagghe, Yangyang Liu, Yinlin Mu, Lin Yang, Xuewen Wang, Xiangsheng Chen   +7 more
semanticscholar   +1 more source

Design and Synthesis of New Potent Inhibitors of Farnesyl Pyrophosphate Synthase

Current Drug Discovery Technologies, 2014
Predictive QSAR models for the inhibition activities of nitrogen-containing bisphosphonates (N-BPs) against farnesyl pyrophosphate synthase (FPPS) from Leishmania major (LeFPPS) were developed using a data set of 97 compounds. The QSAR models were developed through the use of Artificial Neural Networks and Random Forest learning procedures.
Volodymyr, Prokopenko, Vasyl, Kovalishyn, Michael, Shevchuk, Iryna, Kopernyk, Larysa, Metelytsia, Vadim, Romanenko, Sergey, Mogilevich, Valery, Kukhar   +7 more
openaire   +2 more sources