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Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase [PDF]

Expert Opinion on Drug Discovery, 2016
Farnesyl pyrophosphate synthase (FPPS) catalyzes the condensation of isopentenyl diphosphate with dimethylallyl diphosphate to give rise to one molecule of geranyl diphosphate, which on a further reaction with another molecule of isopentenyl diphosphate forms the 15-carbon isoprenoid farnesyl diphosphate.
Rodriguez, Juan Bautista, Falcone, Bruno Nicolas, Szajnman, Sergio Hernan   +2 more
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Farnesyl pyrophosphate and geranylgeranyl pyrophosphate synthetases during Cucurbita pepo germination

Phytochemistry, 1974
Abstract Although the geranylgeranyl pyrophosphate synthetase activity was very low compared with farnesyl pyrophosphate synthetase activity on imbibition of pumpkin seed, the former increased markedly and the latter decreased as germination proceeded.
Kyozo Ogura, Shuichi Seto
exaly   +2 more sources

Simultaneous determination of farnesyl and geranylgeranyl pyrophosphate levels in cultured cells

Analytical Biochemistry, 2005
A sensitive, nonradioactive analytical method has been developed to simultaneously determine the concentrations of farnesyl pyrophosphate (FPP) and geranylgeranyl pyrophosphate (GGPP) in cultured cells. Following extraction, enzyme assays involving recombinant farnesyl protein transferase or geranylgeranyl protein transferase I are performed to ...
Huaxiang Tong, Sarah A Holstein, Raymond J Hohl   +2 more
exaly   +3 more sources

Farnesyl pyrophosphate synthase

2021
Harry Morrison
exaly   +2 more sources

Enzymic conversion of farnesyl pyrophosphate to squalene

Archives of Biochemistry and Biophysics, 1966
Abstract Squalene synthetase of pig liver has been solubilized and partially purified. This enzyme has a pH optimum of 7.4 and a K m value of 5 × 10 −7 M for farnesyl pyrophosphate. A divalent metal ion, Mg ++ or Mn ++ , and NADPH are required for the conversion of farnesyl pyrophosphate to squalene.
G, Krishna, H W, Whitlock, D H, Feldbruegge, J W, Porter   +3 more
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Photoaffinity Analogues of Farnesyl Pyrophosphate Transferable by Protein Farnesyl Transferase

Journal of the American Chemical Society, 2002
Farnesylation is a posttranslational lipid modification in which a 15-carbon farnesyl isoprenoid is linked via a thioether bond to specific cysteine residues of proteins in a reaction catalyzed by protein farnesyltransferase (FTase). We synthesized analogues (3-6) of farnesyl pyrophosphate (FPP) to probe the range of modifications possible to the FPP ...
Kareem A H, Chehade, Katarzyna, Kiegiel, Richard J, Isaacs, Jennifer S, Pickett, Katherine E, Bowers, Carol A, Fierke, Douglas A, Andres, H Peter, Spielmann   +7 more
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Expression of farnesyl pyrophosphate synthase is increased in diabetic cardiomyopathy

Cell Biology International, 2021
AbstractFarnesyl pyrophosphate synthase (FPPS)‐catalyzed isoprenoid intermediates are involved in diabetic cardiomyopathy. This study investigated the specific role of FPPS in the development of diabetic cardiomyopathy. We demonstrated that FPPS expression was elevated in both in vivo and in vitro models of diabetic cardiomyopathy.
Zhengwei Li, Jiefang Zhang, Min Wang, Fuyu Qiu, Chongyin Jin, Guosheng Fu   +5 more
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FORMATION OF A NONALLYLIC HOMONERYL PYROPHOSPHATE BY FARNESYL PYROPHOSPHATE SYNTHETASE

Chemistry Letters, 1975
Abstract The reaction of 4-methylpent-4-enyl pyrophosphate (1) with dimethylallyl pyrophosphate (2) catalyzed by farnesyl pyrophosphate synthetase (prenyltransferase) results in an exclusive cis condensation to give a nonallylic homoneryl pyrophosphate (3).
Akio Saito, Kyozo Ogura, Shuichi Seto
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Inhibition of squalene synthetase by farnesyl pyrophosphate analogs

Journal of Medicinal Chemistry, 1977
The pyrophosphates of the following farnesol analogues have been synthesized: 2-methylfarnesol; 7,11-dimethyl-3-ethyl-2,6,10-dodecatrien-1-ol; 3-demethylfarnesol; 4-methylthiofarnesol; 7,11-dimethyl-3-iodo-2,6,10-dodecatrien-1-ol; 7,11-dimethyl02-iodo-2,6,10-dodecatrien-1-ol; 7,11-dimethyldodeca-6,10-dien-2-yn-1-ol; phytol; 3,7,11-trimethyl-2-dodecen-1-
P R, de Montellano, J S, Wei, R, Castillo, C K, Hsu, A, Boparai   +4 more
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Properties of farnesyl pyrophosphate synthetase of pig liver

Archives of Biochemistry and Biophysics, 1965
Abstract The isolation and partial purification of farnesyl pyrophosphate synthetase of pig liver are described. This enzyme does not have isopentenyl pyrophosphate isomerase, geranyl pyrophosphate synthetase, or geranyl geranyl pyrophosphate synthetase activities.
C R, Benedict, J, Kett, J W, Porter
openaire   +2 more sources