Proteins > Farnesyl pyrophosphate synthase
Page last updated: 2024-08-07 15:58:36
Farnesyl pyrophosphate synthase
A farnesyl pyrophosphate synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14324]
Synonyms
FPP synthase;
FPS;
EC 2.5.1.10;
(2E,6E)-farnesyl diphosphate synthase;
Dimethylallyltranstransferase;
2.5.1.1;
Farnesyl diphosphate synthase;
Geranyltranstransferase
Research
Bioassay Publications (32)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (28.13) | 29.6817 |
| 2010's | 23 (71.88) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| isopentenyladenosine | Homo sapiens (human) | Kd | 1,497.5000 | 4 | 4 |
Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Novel bisphosphonates with antiresorptive effect in bone mineralization and osteoclastogenesis.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 25, Issue:5, 2015
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.ACS medicinal chemistry letters, , Mar-12, Volume: 6, Issue:3, 2015
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
Thienopyrimidine bisphosphonate (ThPBP) inhibitors of the human farnesyl pyrophosphate synthase: optimization and characterization of the mode of inhibition.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site 'capping' phenyls.Bioorganic & medicinal chemistry, , Sep-15, Volume: 20, Issue:18, 2012
Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
Farnesyl pyrophosphate synthase enantiospecificity with a chiral risedronate analog, [6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501): Synthetic, structural, and modeling studies.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Discovery of Lipophilic Bisphosphonates That Target Bacterial Cell Wall and Quinone Biosynthesis.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.Journal of medicinal chemistry, , 12-12, Volume: 62, Issue:23, 2019
Novel bisphosphonates with antiresorptive effect in bone mineralization and osteoclastogenesis.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Fluorescent Farnesyl Diphosphate Analogue: A Probe To Validate trans-Prenyltransferase Inhibitors.Biochemistry, , Aug-09, Volume: 55, Issue:31, 2016
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 25, Issue:5, 2015
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.ACS medicinal chemistry letters, , Mar-12, Volume: 6, Issue:3, 2015
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
Chemo-Immunotherapeutic Anti-Malarials Targeting Isoprenoid Biosynthesis.ACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 54, Issue:17, 2011
Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.ACS medicinal chemistry letters, , Mar-12, Volume: 6, Issue:3, 2015
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 25, Issue:5, 2015
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
3-D QSAR investigations of the inhibition of Leishmania major farnesyl pyrophosphate synthase by bisphosphonates.Journal of medicinal chemistry, , Nov-20, Volume: 46, Issue:24, 2003
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.Journal of medicinal chemistry, , Nov-29, Volume: 50, Issue:24, 2007
Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase--parallel synthesis of analogs via a trimethylsilyl ylidene intermediate.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| dimethylallyltranstransferase activity | molecular function | Catalysis of the reaction: dimethylallyl diphosphate + isopentenyl diphosphate = diphosphate + geranyl diphosphate. [EC:2.5.1.1] |
| geranyltranstransferase activity | molecular function | Catalysis of the reaction: geranyl diphosphate + isopentenyl diphosphate = 2-trans,6-trans-farnesyl diphosphate + diphosphate. [EC:2.5.1.10, RHEA:19361] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 3 target(s):
| Target | Category | Definition |
|---|
| cholesterol biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:ai] |
| geranyl diphosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of geranyl diphosphate. [GOC:mah, MetaCyc:PWY-5122] |
| farnesyl diphosphate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of farnesyl diphosphate. [GOC:jl] |